Somatotropic Hormone;

Acts on target tissues (esp liver) through JAK2 (a TK) to initiate signalling pathways;

Production of IGF-1(&2) to exert effects;

↓ insulin sensitivity, ↑ lipolysis, ↑ protein synth, ↑ epiphyseal growth;

Secretion stimulated by hypoglycemia, insulin;

Physiologic pulsatile release

hGH;

Replacement therapy in children;

Tx: Pituitary dwarfism (in kids most effective if given early, d/c when growth stops);

Tx in adults: reduce CV dz mortality, AIDS-associated wasting;

SE: Kids (fewer) - leukemia (don't give w/i 2 years of tx for cancer), ↑ ICP (intracranial HTN), nausea;

SE: Adults - Peripheral SE: carpal tunnel, peripheral edema, arthralgia, myalgia;

CI: with cancer tx

D2 receptor agonist;

Suppresses prolactin release from the anterior pituitary;

↑ affinity/ ↑ t1/2 compared to Pergolide;

Tx: Hyperprolactinemia from pituitary adenoma

Somatostatin analog, most widely used;

Inhibits insulin, glucagon, GH, and TSH release;

3x daily injections- Short t1/2;

Tx: Insulinomas, glucagonomas, acromegaly, gigantism;

SE: diarrhea, nausea, abdominal pain;

Long acting prep (Sandostatin-LA) now availible (1 injection every 4 weeks)

FSH + LH prep;

Extracted from post-menopausal urine;

IM admin (are peptides);

Tx: Female infertility

GnRH analog;

Longer t1/2, better receptor binding - induces receptor downregulation;

Admin is pulsitile via IV pump;

Tx: Reproductive disorders secondary to reduced GnRH;

SE: Phelbitis at pump site;

Not approved for use in men (gonadotropins are prefered in men. Gonadotropins in women=risk of multiple pregnancies)

Synthetic ACTH - a corticotropin (24 AA);

Binds a membrane receptor and exerts actions via adenylate cyclase activation and cAMP ↑;

Preferred to natural product (HP Acthar Gel isolated from animal adrenals) b/c the synthetic lacks the contamination which = vasopressin activity;

Use: test integrity of HPA axis (only real clinical use of ACTH) - inject (IM/IV) Cosyntropin and measure cortisol at 30 and 60 mins (spike in cortisol means there are functional ACTH receptors in the adrenal cortex - Z. fasiculata)

Glucocorticoid (hydrocortisone);

Long t1/2;

Oral, topical, inhaled admin;

Tx: bronchial Asthma, skin irritation

Adrenocortical "inhibitor";

Inhibits CYP450scc (side chain cleavage, first step in cortisol synthesis from cholesterol) - Decreases cortisol production;

Tx: Cushings (inhibits cortisol overproduciton)

Estrogen - synthetic 17alpha;

Addition of ethinyl (triple bonded) ↓ first pass met;

General Estrogen Effects: ↑ HDL/↓ LDL, induce epi plate closure, antagonize bone resorption/clast activity, ↑ libido, induces synth of TBG, transcortin, SHBG, and clotting factors from the liver, and stimulates the progression of endometrial/breast tumors;

Tx: CONTRACEPTION (most common Rx);

SE: ↑ risk of thromboembolism, ↑ breast size, excitement

Synthetic progesterone;

Progesterone actions: maintenance of pregnancy, development of breast ductal system, inhibition of uterine contraction, elevation of basal insulin levels (glycogen storage), ↓HDL/↑ LDL, stim lipoprotein lipase, ↑ temp in ovulation;

Tx: Endometrial cancer, progesterone component of many birth control and morning after products;

SE: ↑ risk of cardio disease, acne, weight gain

SERM;

Tissue selective! Estrogen Agonist in bone, brain, liver,

Antagonist in breast, endometrium - blocks only where you need it to!;

Tx: Breast & endometrial cancers

(Blocks the estrogen stimulation of cancers while maintaining normal fxn elsewhere)

SERM;

Tissue selective! Estrogen Agonist in bone, brain, liver,

Antagonist in breast, endometrium;

Tx: Breast & endometrial cancers (blocks estrogen stimulation of cancers w/o effecting other tissues)

True Anti-estrogen;

Antagonist in all estrogen receptors (ER-alpha & -beta);

Ovulation induction via reflex inc GnRH;

Tx: Infertility (via ovulation induction);

Anti-estrogen;

Antagonist in all tissues (ER-alpha & -beta);

Ovulation induction via reflex inc GnRH (blocks estrogen feedback on the hypothalamus);

Tx: Ovulation induction to tx Infertility

Anti-progestin;

Blocks Progestin receptor for the termination of gestation in first 7 weeks;

Abortifacient

Aromatase inhibitor;

Blocks the conversion of androgens to estrogens,

Decreases estrogens to very low levels;

Tx: Breast cancer after Tamoxifen fails

Androgen;

[A] Bind androgen receptor - transcriptional regulation; [B] Conv to DHT - which has ↑ potency;

[C] Conv to estradiol - closes epiphyseal plates;

Tx: Elderly men (↑ muscle mass), IM injection for HRT, endometriosis, PMS, anabolic steroids;

SE: Masculinization/virilization, Edema*, Cholestatic hepatitis (jaundice, esp with alkylated products), Priapism, CAD, hepatic carcinoma (HCC), suppression of LH & FSH release (reduces spermatogenesis)

Testosterone derivatve;

Oral, short acting;

[A] Binds androgen receptor - transcriptional reg;

[B] Conv to DHT - ↑ potency;

[C] Conv to estradiol - closes epiphyseal plates;

Tx: Elderly men (↑ muscle mass), IM injection for HRT, endometriosis, anabolic steroids;

SE: ↑ CHD risk, virilizing in women (excess T), feminizing in men (dt conversion to estradiol), suppression of FSH/LH (↓ endogenous T production, spermatogenesis, testicular size), edema, cholestatic hepatitis, prapism, hepatic carcinoma

Testosterone derivatve;

IM, long acting;

[A] Binds androgen receptor - transcriptional reg;

[B] Conv to DHT - ↑ potency;

[C] Conv to estradiol - closes epiphyseal plates;

Tx: ENDOMETRIOSIS*, PMS (advantage here bc this drug is only weakly androgenic*),

In elderly men (↑ muscle mass), IM injection for HRT, anabolic steroids;

SE: CHD, Virilizing/Feminizing, reduced testis size/spermatogenesis/endogenous T production, edema, cholestatic hepatitis, priapism, hepatic carcinoma.

Androgen receptor antagonist;

Competes with DHT;

Tx: Acne, baldness, virilizing syndrome, sexual deviants (reduces libido)

Androgen receptor antagonist;

3x daily dosing;

Tx: Prostate cancer;

SE: Hepatotoxic*

(Propecia);

Blocks testosterone conversion to DHT (5 alpha reductase inhibitor);

Tx: BPH, male-pattern baldness;

SE: Teratogenic (pregnant women really shouldn't even touch this drug, adverse effects especially on a Male fetus)

1st Gen. Sulfonylurea;

Oral admin (1-2x daily), rapidly absorbed, extensive protein binding;

Acts @K+ channel;

Initially ↑ insulin release (not a long term effect);

↑ insulin sensitivity by enhancing the effect of insulin on ↑ glucose uptake;

Tx: DM, promote hypoglycemia;

NSAIDs enhance the hypoglycemic action of sulfonureas

1st Gen. Sulfonylurea;

Oral admin (1-2x daily), rapidly absorbed, extensive protein binding;

Acts @K+ channel;

Initially ↑ insulin release (not a long term effect);

↑ insulin sensitivity by enhancing the effect of insulin on ↑ glucose uptake;

Tx: DM, promote hypoglycemia;

NSAIDs enhance the hypoglycemic action of sulfonureas

2nd Gen Sulfonylurea-10-100X more potent than 1st;

Oral admin (1-2x daily), rapidly absorbed, extensive protein binding;

Acts @K+ channel;

Initially ↑ insulin release (not a long term effect);

↑ insulin sensitivity by enhancing the effect of insulin on ↑ glucose uptake;

Tx: DM, promote hypoglycemia;

NSAIDs enhance the hypoglycemic action of sulfonureas

Meglitinide - benzoic acid derivative- oral hypoglycemic;

Very rapid GI absorption;

↑ insulin secretion;

Short t_1/2, used to lessen the post-prandial glucose spike (take before* each meal);

Tx: DM, promote hypoglycemia;

SE: Severe hypoglycemia*;

Biguanide oral hypoglycemic agent;

GI absorption - little first pass metabolism;

Activates AMP-stimulated protein kinase and specifically ↓ hepatic glucose production;

Also inhibits hepatic and renal gluconeogenesis, stim gulcose uptake/glycolysis in the periphery, slows glucose abs form the GI, and ↓ plasma glucagon levels;

No hypoglycemia, NO INSULIN AXN, no weight gain;

Tx: Type II DM;

SE: GI disturbance and

BLACK BOX warning for lactic acidosis;

Can be given in combo with Glyburide (2nd gen sulfonuria drug with insulin effects)

Thiazolidindione;

GI absorption - little first pass metab;

Binds the PPARγ receptor = ↓ insulin resistance in the liver and peripheral tissues. ↓ withdrawal of glucose from the liver;

Reduces quantity of glucose, insulin and glycated Hb in the bloodstream;

In sum: ↑ insulin sensitivity;

Tx: DM, promote hypoglycemia;

SE: Fluid retention/edema/weight gain, anemia, bone fractures in women, may worsen cardiac disease.

Oral hypoglycemic agent;

Intestinal Alpha-glucosidase inhibitor;

↓ carbohydrate (starch) abs by preventing the breakdown of carbs;

↓ post-prandial glucose spike;

Tx: DM, promote hypoglycemia;

SE: GI disturbances;

Used in combo with other drugs*

Parenteral hypoglycemic agent;

Synthetic Incretin (GLP-1 analog)- Works thru GIP/GLP-1 mechanisms, (more potent) to improve glycemic control;

↑ insulin secretion in response to glucose, ↓ glucagon stimulated glycogenolysis, slows gastric emptying, ↓ appetite, ↓ glucagon, some ↑ in beta cells = hypoglycemia/reduced rise in post-prandial blood glc;

SE: GI, HA, Pancreatitis*

Calcitriol mimetic;

Converted in the body to calcitriol;

Tx: Rickets, osteomalacia, hypoparathyroid, osteoporosis

Calcitriol analog;

Tx: PSORIASIS (better than glucocorticoids), rickets, osteomalacia, hypoparathyroid, osteoporosis

1st Gen. Bisphosphonate;

Less effective orally (oral admin is tough but done) - Take in am, without food and with a full glass of water;

Analog of inorganic pyrophosphate - inhibits bone resorption;

Tx: Pagets Dz*, osteoporosis, (tx hypercalcemia only when given by IV infusion);

SE: If via IV admin (not the common use but can tx hypercalcemia), osteonecrosis of jaw (not common in 1st gen)

Fosamax;

2nd Gen. Bisphosphonate - more potent;

MC Rx for post-meno Tx;

Analog of inorganic pyrophosphate - inhibits bone resorption;

Take in am, without food and with a glass of water;

Tx: Pagets, osteoporosis (post-menopausal);

SE: via IV admin, osteonecrosis of jaw (not common in 2nd gen), irritation of esophagus

3rd Gen. Bisphosphonate - HIGH POTENCY;

Analog of inorganic pyrophosphate - inhibits bone resorption;

Take in am, without food, with water;

Tx: Pagets, osteoporosis, Lytic Bone Cancers (prostate and breast - 3rd gen only);

SE: via IV admin, osteonecrosis of jaw (common in 3rd gen drugs)!

3rd Gen. Bisphosphonate - HIGH POTENCY;

Analog of inorganic pyrophosphate - inhibits bone resorption;

Take in am, without food, with water;

Tx: Pagets, osteoporosis, Lytic Bone Cancers (prostate and breast - 3rd gen only);

SE: via IV admin, osteonecrosis of jaw (common in 3rd gen drugs)!

Calcimimetic - Ca sensing receptor mimetic;

Binds allosterically to the calcium sensing receptor (CaSR) in the parathyroid gland and allows PTH suppression at lower actual [Ca2+], suppresses PTH/effectively ↓ circulating PTH;

Tx: Hyperparathyroidism in pts with parathyroid carcinomas;

Anti-Protozoal;

Prodrug- requ activation by sensitive organisms = enzymatic reduction;

Blocks pyruvate:ferrodoxone oxidoreductase;

90% bioavail, BBB penetration, low protein binding;

Oral admin;

Tx: Trichomonas, Entamoeba, Giardia, anaerobes (B. fragilis, C. diff);

SE: GI, HA, metallic taste*, dizziness, disulfriam-like reaction*, anorexia, neuro tox;

CI: in pt with CNS dz (dizziness, vertigo, neuropathies) and in pregnant women (teratogenic*);

Interactions: Metronidazole inhibits the secretion of Lithium and of Coumadin (toxicity and ↑ PT)

Anti-Protozoal;

Inhibits electron transport chain = ↓ pyrimidine synth; 99% protein bound, lipophillic, hydrophobic - enterohepatic reciculation;

Tx: Pneumocystic pneumonia (PCP)*, Toxoplasma, Entamoeba, Trichomonas, P. falciparum;

Few SE: rash, nausea possible

Anti-Protozoal;

Oral (50% bioavail) or IV admin;

Inhibits ornithine decarboxylase to block polyamine synthesis;

Tx: West trypanosoma (East has less stable ODC, not as good a target);

SE: Anemia & leucopenia*, diarrhea, convulsions, GI, alopecia;

Thereputic dosage is large and requires concurrent admin of IV fluids, may lead to fluid overload.

Antimalarial - Blood schizontocide;

Wide distribution, slow clearance (months to years)*;

Resistance: efflux at P-gp*;

Tx: Plasmodium, non-GI (extraintestinal-doesn't stay in the GI)* amebiasis;

Prophylactic use;

SE (dt concentration of this drug in melanin-containing cells*): blurred vision (corneal deposits), retina pigmentation, hemolysis (if G6PD deficient pts*), ototoxicity, myopathy, and peripheral neuropathy with high doses;

Anti-malarial - Blood schizontocide;

Binds to DNA and blocks DNA synthesis;

Tx: P. falci (blood), gametes of P. vivax and P. malariae;

Poor therapeutic index - worst of all antimalarials;

SE: ↓ cardiac contractility, dilates vessels, contracts the uterus, vertigo, hemolysis (if G6PD deficient), Cinchonism - tinnitus, blurred vision, HA, ↓ hearing;

CYP inducers ↓ half life of this drug and req ↑ dose;

Antimalaria- Blood schizontocide;

Oral admin, 98% bound, excreted in bile;

Acts only @ asexual erythrocytic stages;

Blocks DNA synthesis;

Tx: P. falci, gametes of P. vivax and P. malariae;

SE: GI, vertigo, convulsions;

CI: BBs, chloroquine, quinine, quinidine, hx seizures

Tetracycline (30S ribosome binding and inhib);

Anti-protozoal -Antimalarial - Blood schizontocide* and Abx;

Attacks plasmodia in RBC preventing or terminating the clinical attack;

Acts only @ asexual erythrocytic stages;

Antimalarial - Tissue schizontocide;

Gametocidal, Hypnozoitocidal;

Take with food*;

Rapidly abs and conv to Carboxyprimaquine;

Tx: Prophylaxis, P. vivax and P. ovale @ hepatic and gamete stages;

KILLS P. FALCI GAMETES;

Good Thereputic Index;

CI: G6PD deficient (X-linked) = hemolytic anemia, avoid long term use (risk of toxicity and sensitization)

Antimalarial - Tissue schizontocide;

High abs - concentrates in RBC, Crosses the placenta, distributed in breast milk;

Inhibits DHFR;

Tx: P. falciparum in combo (does not tx vivax);

SE: Rash, ↓ hematopoeisis, megaloblastic anemia (w prolonged therapy);

Never used alone* often combined w/ Sulfadoxine

Benzimidazole - Anti-helmintic;

Rapid met to albendazole sulfoxide;

Inhibits MT assembly - immobilization and death;

Blocks larval development;

Tx: helmintics - ascariasis, enterobius, hookworm;

SE: teratogen

Benzimidazole - Anti-helmintic;

Poor abs, highly bound;

Inhibits MT assembly - immobilization and death;

Blocks larval development;

Tx: helmintics - ascariasis, enterobius (pin), Trichuris (whip), hookworm (broader spectrum than Alben);

SE: Minor GI distress, Teratogen

Anti-helmintic;

↑ membrane permiability to Ca/cations -spastic paralysis;

Readily abs, hi first pass met, ↑↑ metabolites;

Tx: tapeworms, schistosomiasis, 3 forms of fluke (lung, liver, and intestinal);

SE: GI, HA;

CI: Carbamazepine & Phenobarbital ↓ bioavail; Cimetidine ↑ bioavail, Don't give to pt with ocular schistosomiasis**;

Anti-helmintic;

Oral admin, no met, long t1/2 (slow cl);

↑ Cl permiability of parasite membrane - inhibiting glutamate and GABA-ergic channels - paralysis;

Tx: strongyloidiasis, onchocerca (rvr blindness);

SE: GI, itch, dizzy, inflamm rxn to dying bugs*

Anti-helmintic;

Rapid GI abs;

MOA Unknown;

Tx: lymphatic filariasis;

SE: (relatively severe) anorexia, nausea, HA, and major reactions to the destruction of microfilariae by the host.

Anti-helmintic;

Poor abs; Binds Nicotinic receptors - depol blockade - spastic paralysis (bug falls off GI wall);

Tx: MONILIFORMIS (DoC), GI nematodes;

↓ SE dt localization of drug in GI - HA, dizziness, rash

Bile acid sequesterant - Powder form;

Anionic compound binds - charged bile acids in GI - inhibits enterohepatic bile recycling (strong ion exchange resin) - liver excretes more cholesterol;

Safe for children and pt with hepatic dz;

↓ LDL by 25% but ↑ TGs*, no real effect in HDL;

SE: Sandy texture, flatulence, hypertriglyceridemia, constipation, fecal impaction, many drug interactions;

CI: In pt with complex or vital drug regimens and pt with hypertriglyceridemia.

HMG-CoA Reductase inhibitor - Statin;

Prodrug, intestinal abs by P-gp;

Inhibits cholesterol synthesis in liver - ↑ # of LDL receptors - ↑ clearance of VLDL and LDL from blood;

↓ LDL by 60% (dose dep), ↑HDL (not dose dep), ↓ TGs;

SE: GI, sleep disruption, teratogenic*, myalgia, myositis, rhabdomyolysis* (↑ CPK, acute renal failure), ↑ aminotransferases,

Interactions @ CYP3A4* and drugs that inhib P-glycoprotein mediated intestinal abs (Cyclosporine, Grapefruit juice, Gemfibrozil (req ↓ dose);

Cautions: Renal dz (reduce dose)

HMG-CoA Reductase inhibitor - Statin;

Prodrug, intestinal abs by P-gp;

Inhibits cholesterol synthesis in liver - ↑ # of LDL receptors - ↑ clearance of VLDL and LDL from blood;

↓ LDL by 60% (dose dep), ↑HDL (not dose dep), ↓ TGs;

SE: GI, sleep disruption, teratogenic*, myalgia, myositis, rhabdomyolysis* (↑ CPK, acute renal failure), ↑ aminotransferases,

Interactions @ CYP3A4* and drugs that inhib P-glycoprotein mediated intestinal abs (Cyclosporine, Grapefruit juice, Gemfibrozil);

No dose adjustment in renal dz or with Gemfibrozil*** Do have to limit dose with CYP drugs and Cyclosporines.

Cholesterol absorption inhibitor; Blocks sterol-induced internalization of NPC1L1 by blocking association with clathrin/AP2 complex;

↓ cholesterol abs by 50% - ↓ hepatic cholesterol - upregulation of LDL-R = ↓ LDL by 18%;

↓ LDL, ↑ HDL, ↓ TGs;

SE: GI, fatigue, gallstones*, Category C in preg, ↑ liver enzymes; Higher lvls in elderly, female pts;

CI: age <10 yrs, hepatic or renal insuff, lactation*

Mechanism is complementary to statins and they are often combined (Vytorin = combo pill)

Fibrate - anti-lipid/hypercholesterolemia drug;

Active metabolite = fenofibric acid - glucaronidation; Activates PPARα nuclear receptor (liver, muscle, kidney, heart) = FA oxidation, ↑ biliary cholesterol excretion;

↓TG by 50%, ↑ HDL (Apo-A1), no effect on LDL!;

↓ CHD in pts with metabolic syndrome*

SE: Gallstones*, ↑ transaminases, ↓ GFR, azotemia;

CI: Renal dz* (drug accumulates and ↑ Cr)

Synthroid = L-T4;

Most common Rx;

Calorigenic, ↑ HR/cardiac contraction force;

Tx: Hypothyroidism;

Larger doses must be used in kids, takes several weeks to reach steady state (carefully monitor levels as small changes in hormonal levels can make a big difference).

L-T4 and L-T3;

Calorigenic, ↑ HR/cardiac contraction force;

Mixture is not prefered due to variability in levels.

[PTU] Thioureylenes - anti-thyroid;

[1] Inhibits I organification (via peroxidases), can't bind to thyroglobulin;

[2] Inhibits peripheral (liver) conversion of T4→T3;

Tx: Hyperthyroidism;

SE: Agranulocytosis, rash;

Less likely to cross placenta, use caution but DoC in pregnancy*** (PTU in PG)

Thioureylenes - anti-thyroid;

Inhibits I organification(via peroxidases), can't bind to thyroglobulin;

10X more potent and longer t1/2 than PTU;

Tx: Hyperthyroidism;

SE: Teratogen, CI in Pregnancy

Oral admin;

Concentrates in the thyroid, beta-radiation will destroy parenchymal cells, minimum collateral damage;

Adult usage, but not in women of child-bearing age;

Tx: enlarged thyroid (Graves, goiter)

Iodinated contrast medium;

Inhibits peripheral (liver, kidney, pituitary, brain) conversion of T4→T3;

Off Label Tx: Hyperthyroidism

Marijuana;

Delta-9-THC psychoactive compound;

Cannabinol (CBN) = less active metabolite, cannabidiol (CBD) = anxiolytic;

Retrograde transmission - ↑ extracellular K, blocks Ca++ influx, ↓ NT release, ↓ cAMP = leads to tolerance;

SE: Psychotoxicity (schizophrenia), carcinogenic (SCC), teratogenic*

Acute - ↓ memory, confusion, depersonalization, ↑ hunger, ↓REM, ↓ balance, dry mouth;

EARLY High: Euphoria, laughter, time distortion;

LATE high: relaxation, introspection, dream like state;

Chronic: amotivational syndrome, apathy, dullness, ↓concentration, ↓memory;

Tolerance: ↓ adenylate cyclase (cAMP), ↓ receptors (CB1 - basal ganglia, limbic, cerebellum, hippocampus, nucleus acumbens, and CB2 - immune/spleen);

Cross tolerance with opiods and EtOH*

↓ T-cells;

Suppress immune response Via CB2 receptor on lymphocytes and macrophages

↓ LH and FSH;

↓ testosterone, testes ♂, ↓ libido;

↓GH, ↓ Prl, ↑ACTH; Anovulatory cycles ♀

Medical marijuana;

NATURAL product extracted THC - 7TM cannabinoid receptor agonists - GPCR, Gi = ↓ cAMP by inhibition of Adenylate cyclase > Blockage of Ca2+ entry into the cell, and ↑ extracellular K+;

Approved Use: Antiemetic during chemo, and to txAIDS wasting syndrome;

Possible uses - MS, spinal injury, Tourette's, dyskinesias

LSD - Hallucinogen;

5-HT2 partial agonist;

Physiological sx = sympathomimetic;

Psychic = Visual hallucinations, time/sense alteration, loss of boundaries, emergence of thoughts/memories, 'magically in control', synesthesia;

Rapid tolorance*

SE: Bad trip (prolonged psychosis), sober flashbacks

Mescaline

3,4,5-trimethoxyphenethylamine

Peyote (cactus containing Mescaline Peyote Buttons); Hallucinogen - Psychedelic alkaloid;

5-HT and DA agonist;

Physiological  - Sympathomimetic;

Psychic - hallucinations, unusual time perception;

SE: paranoia and fear*;

Schedule 1 drug

Nicotine gum;

24% abs @ 6 mos 18% abs @ 1 yr;

Terminate use after 6 mo.;

Best efficacy in combination with cessation programs and pharmacologic aids e.g. zyban;

Must retain in mouth for 2-30 minutes. Do not swallow;

CI: oral lesions, active smoking

Nicotine Transdermal Patch;

Variable time to peak plasma concentration: Prostep the longest with peak at 9 hrs;

16.8% abs @ 6 mos;

Well tolerated;

Best efficacy in combination with cessation programs;

SE: sleep disturbance, skin irritation;

CI: active smoking (additive fx)

Chantix - Non-nicotine cessation compound;

Nicotine receptor partial agonist;

High affinity @ alpha4-beta2 nicotine receptors, some affinity @ 5HT-3;

25% @ 12 mos abstinence, 2nd line tx after Buproprion

SE: Mood changes, nausea (MC);

BB warning suicidal ideation

Non-nicotine cessation aid (old Anti-HTN medication); Non-selective antagonist a non-alpha7-Nicotinic cholinergic receptors;

Crosses BBB;

Action @ brain and peripheral ganglia - ↑ SE's; Inconclusive efficacy, use w/ patch;

NMDA antagonist, alters ion channels – initially excitatory then depressive;

Diff channels effected at diff concentrations of intox; Detox requires ADH and ALDH enzymes;

Women have ↓ gastric first pass metabolism and ↓ ADH levels = increased risk of tox;

SE: CNS damage, hepatomegaly, vasodilation, cardiomyopathy, pancreatitis* (acute and chronic), anemia (megaloblastic and sideroblastic), bone marrow suppression, teratogenic;

CI: with NSAIDs (potentiates teh gastric damage)

Thiamine B1 deficiency - Beriberi;

Wernicke's encephalopathy - nystagmus, ocular palsies, ataxia, gait;

Korsakoff's psychosis - Konfabulation -perminant CNS damage;

Antero and retrograde amnesia;

Cerebellar degeneration - ataxia;

Pontine myelinolysis - dysarthria, confusion;

Marchiafava-Bignami - apathy, Alz-like dementia, movement disorders;

Pellagra-Niacin B3 deficiency – 5 Ds (incl dementia, diarrhea and dermatitis);

Hepatic encephalopathy (ammonia increase);

Peripheral neuropathies,

Direct CNS toxicity

Early: agitation, confusion, hyperactive ANS, seizure(2-48hrs)

Late: DTs- hyperthermia, hallucination, disorientation; Coma, death;

Tx: BNZ, phenytoin, Phenobarbital (siezures) atenolol (tx early tremors, and delirium/DTs*), clonidine

Wood alcohol;

Oxidized to form FORMALDEHYDE(!) and formic ACID;

SE: blindness, irreversible acidosis, death;

Tx: OD w/ ethanol (competitive substrate) and dialysis, treat acidosis

Other anticdote (added to the block list) : Fomepizole (tx both methalol and ethylene glycol poisoning)

Vitamin B1;

Should admin to all alcoholics in distress;

Replacement for thiamine lost in deficient state;

Deficiency is Beriberi Wet=CV complications  or Dry=CNS complications;

B1 is required for myelination and is invloved in carbohydrate (CHO) metabolism;

(ALDH) Acetylaldehyde dehydrogenase antagonist - ↑ acetaldehyde;

Inhibits DA beta-hydroxylase (↓ NE);

Induces Acetaldehyde Syndrome - ↑ HR, flushing, hypotension, N/V, HA;

No effect on cravings;

Tx: Chronic alcoholism;

SE: hepatotoxcity, depression, psychosis

Opioid receptor antagonist;

Long Duration of axn (24 hrs), effect t_1/2=4 hrs;

Oral admin (extensive first pass) or Depot;

Tx: Alcohol abuse (↓ craving and ↓ relapse*, ↓ number of 'heavy drinking days'), and Opiate OD (but caution, precipitates withdrawl);

Zofran;

Anti-emetic - 5-HT3 antagonist;

↓ alcohol cravings by blocking the reward pathway;

Tx: chronic alcoholism, nausea;

Note that use in alcoholism tx has been shown in early onset alcoholism only, not late*

AMPA-R antagonist, GABA-R regulator;

Tx: Migraines, seizures, off label to tx Chronic alcoholism (↓ # of 'heavy drinking days');

Need to titrate dosing;

SE: visual impairment/glaucoma (rare), cognitive difficulties;

Beta-1 antagonist;

Tx: EtOH withdrawal stages... tremulousness syndrome, early tremors, DTs, and delirium*

Basically everything but the seizures that may occur late;

Rengenerates glutathione;

Oral or IV;

Tx: Acetaminophen OD when >[150mg/mL] @ 4hrs OR >[75mg/mL] @ 8 hrs, can also tx Asprin OD (?);

Use in first 10 hrs;

SE: anaphylaxis, N/V, taste/odor;

Benzodiazepine antagonist (works with BNZ receptor agonists but not with Barbituates;

Tx: BNZ OD;

Can produce withdrawal symptoms, not used too often*;

SE: N/V, dizzy, panic attacks, blurred vision, seizures*

Reversible anticholinesterase inhibitor;

Tx: Atropine O.D., and OD with other anticholinergic (antidepressant, antihistamine, antiemetic, antipsychotic) agents;

SE: Bradycardia, seizures*;

CI: TCA's (can cause heart block)

Anticholinergic;

Tx: Organophoshate (insecticides, parathion, malathion, diazinon and Carbamates - aldocarb, carbofuran, isolan = nerve gas) OD - all of which inhibit breakdown of Ach causing overstimlation and respiratory failure;

Use with supportive tx

Reactivator of cholinesterase;

Slow IV admin;

Tx: Organophosphate, sarin, soman OD!;

Rapid admin SE's: NM block, msucle spasm, HTN, tachycardia

Chelator;

Tx: Lead poisoning in children, also tx mercury and Arsenic poisoning;

Reduces blood levels but does not reverse damage done by toxins;

SE: Hypersensitivity;

Hydration is key - renal excretion;

Chelator;

First line tx for arsenic poisoning*;

Also Tx lead and mercury poisoning;

SE - nephrotoxic;

CI - G6PD deficiency - hemolysis

Iron poisoning? Don't reamin inDEFERent to tx!*

Iron chelator;

Tx: First line for iron tox;

SE: Red urine*, tachycardia, hypoT, abdominal pain, N/V, flushing, fever

TCA (tertiary amine);

Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation, blocks mAch, 5-HT, and Histamine receptors*;

Very sedating + Anticholinergic effects (most);

High lipid solubility; Low therapeutic index;

Tx: Depression, anxiety (OCD), ADHD; 

SE: Orthostatic hypoT, tachycardia, confusion, anticholinergic*, worsens narrow-angle glaucoma and CHF, acidosis, delirium, seizures*;

CI: Additive CNS depression (EtOH, hypnotics)

TCA (tertiary amine);

Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation, blocks mAch, 5-HT, and Histamine receptors*;

Very sedating + Anticholinergic effects;

High lipid solubility; Low therapeutic index;

Tx: Depression, anxiety (OCD), ADHD, nocturnal enuresis; 

SE: Orthostatic hypoT, tachycardia, confusion, anticholinergic*, worsens narrow-angle glaucoma and CHF, acidosis, delirium, seizures*;

CI: Additive CNS depression (EtOH, hypnotics)

 CYP2D6, conjugation = ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine

TCA (secondary amine);

Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation;

Blocks mAch - no 5-HT effect, little Histamine effects;

Low sedation*;

High lipid solubility, low thereputic index:

Tx: depression, anxiety (OCD), ADHD;

SE: Orthostatic hypoT, tachycardia, confusion, anticholinergics, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures (lowers seizure threshold);

CI: Additive CNS depression (EtOH, hypnotics)

Wellbutrin

Atypical antidepressant;

2nd Generation No sedation No anticholinergic fx;

MOA uncertain, blocks NE reuptake (↑ NE), weak blocker of DAT, SERT, NET;

Oral - divided doses or slow release formulation;

Take in the morning;

Tx: Depression and used as a non-nicotine smoking cessation aid*;

SE: Anxiety, HA, restlessness, seizures (No sexual side effects*);

Atypical antidepressant - 3rd generation;

Presynaptic α-2 receptor antagonist [unique] causing ↑ release of 5-HT and NE; NOT an MDR-1 substrate;

Antagonizes 5-HT2 and 5-HT3 receptors, anti-histamine actons = Strong sedation;

Tx: Depression (in little old ladies who don't eat enough or sleep well);

SE: Sedation, weight gain;

Antidepressant;

Potent anticholinergic, 5-HT reuptake inhibitor;

No NE effect;

INHIIBITS CYP3A4;

Tx: Depression w/ sleep disturbance and/or anxiety;

DC'ed in ost countries in 2003 dt severe hepatotoxicity (some generics still availible)

SSRI - inhibits SERT to potentiate serotonin action;

CNS stimulation, euphoria;

Long t_1/2 = 2-3 days;

High therapeutic index;

Tx: MDD, panic disorder, OCD, ADHD:

SE: Nausea, reduced libido/anorgasmia, Serotonin withdrawl syndrome (taper off);

Has the LEAST side effects of SSRIs;

CI: MAOI (within 2 weeks of SSRIs), amphetamines, ecstasy, LSD, L-tryptophan;

Serotonin Syndrome (hyperthermia, hyperreflexia, tremor, seizures, CV collapse, coma, death);

Prozac;

SSRI - inhibits SERT to potentiate serotonin action;

CNS stimulation, euphoria;

Long t_1/2 = 1 week*;

High therapeutic index;

Tx: MDD, panic disorder, OCD, ADHD:

SE: Nausea, reduced libido/anorgasmia, Serotonin withdrawl syndrome (taper off);

CI: MAOI (within 2 weeks of SSRIs), amphetamines, ecstasy, LSD, L-tryptophan;

Serotonin Syndrome (hyperthermia, hyperreflexia, tremor, seizures, CV collapse, coma, death);

 MAY ↑ levels of lithium, warfarin and TCAs*

MAOI

Irreversibly inhibits oxidative metabolism of monoamines (NE, 5-HT) ↑ vesicle stores/amt released;

 Acute effects:CNS Stimulation, agitation euphoria;

Requires daily dosing due to inactivation;

2nd line anti-depressants, also tx - panic disorder, agoraphobia;

 SE: Orthostatic hypoT sleep disturbance, agitation;

CI: Cheeses (tyramine) EtOH, sympathomimetics (beta agonists) = [Acute HTN],

Meperidine, dextromethorpham, SSRIs [Serotonin Syndrome]

Mood-stabilizer;

Unknown MOA - may block inositol P signal/AC activity;

Rapid absorption, NOT metabolized, renal clearance - t1/2 = 20 hrs;

Narrow thereputic window*;

First line tx: Bipolar disorder, also tx manic depressive disorder;

 SE: Tremor, ataxia, hyperactivity, aphasia, sedation, edema, hypothyroid, nephrogenic DI, cardiac sick sinus syndrome [bradycardia], acne, folliculitis, ↑ psoriasis;

Teratogen;

CI: NSAIDS alter renal elimination

Ambien;

BNZ Receptor Agonist (BRA);

Modify the response of GABA receptor to GABA (shift dose response curve L), Req GABA;

Specific for BZ-1 receptor at approved doses;

Tx: Insomnia;

Pregnancy category C (Okay, but caution, unlike BNZ which are Category X);

Schedule IV;

Sonata;

BNZ Receptor Agonist (BRA);

Modify the response of GABA receptor to GABA (shift dose response curve L), Req GABA;

Specific for BZ-1 receptor at approved doses;

Tx: Insomnia;

Pregnancy category C (Okay, but caution, unlike BNZ which are Category X);

Schedule IV;

ETHNIC VARIABILITY - Asians, must ↓ the dose (differences in aldehyde dehydrogenase levels (?))

HIV Fusion Inhibitor;

Prevents viral entry into host cell by binding gp41 of viral envelope and preventing the comf change req;

Admin SQ, 2X a day;

Met by proteolytic hydrolysis, no CYP rxns and no cross resistance with other drugs;

Tx: Experienced HIV pt who are failing HAART;

SE: 8x ↑ risk of bacterial pneumonia*

Nucleoside Reverse Transcriptase Inhibitor (NRTI);

Nucleoside analog (pyrimidine-T);

Competitive inhibitor of viral RT - Blocks elongation in previously uninfected cells;

Req (+P)X3 for axn;

↓ perinatal HIV transmission;

Met by glucaronidation. Avoid fatty meals (↓ AUC);

SE: BM suppression, lactic acidosis with hepatic steatosis (mitochondrial toxicity), lipodystrophy;

Avoid with other drugs that cause myelosuppression;

Nucleoside Reverse Transcriptase Inh (NRTI);

Nucleoside analog (purine-A,G);

Forms active ddATP - act as competitive inhibitor - blocks elongation in previously uninfected cells;

Req (+P)X3 for axn;

Don't take w/ acidic foods (↓ AUC);

SE: Peripheral neuropathy, Pancreatitis, lactic acidosis w hepatic steatosis, lipodystrophy, many drug interaxns

Nucleoside Reverse Transcriptase Inh (NRTI);

Anti-retroviral and Anti-HBV;

Nucleoside analog (pyrimidine-C) acts as competitive inhibitor of viral RT, blocks elongation in previously uninfected cells;

Req (+P)X3 for axn;

Longest NRTI t_1/2;

SE: lactic acidosis with hepatic steatosis, lipodystrophy

Protease inhibitor - Anti-retroviral;

Most effective ART* - competitive, reversible, inhibitor of viral aspartyl proteases (binds protease active site), esp in monocytes/macs - blocks viral maturation;

CYP3A4 Inhibitor - but least in class;

600% ↑ AUC if taken w/ meals;

SE: Hyperlipidemia, DM, lipodystrophy, ↑ liver enzymes, ↑ bleeding in hemophliacs;

Many drug-drug interactions dt CYP inhibition;

Protease inhibitor - Anti-retroviral;

Most effective ART* - competitive, reversible, inhibitor of viral aspartyl proteases (binds protease active site), esp in monocytes/macs - blocks viral maturation;

CYP3A4 Inhibitor - most potent in class;

 SE: Hepatotoxic, hyperlipid, DM, lipodystrophy, ↑ liver enzymes, ↑ bleeding in hemophliacs;

Lots of Drug-Drug interactions dt CYP inhibition;

Anti-Herpes Drug - Nucleoside (Purine) analog;

Inhibits viral DNA polymerase by direct binding and by causing chain termination;

Req (+P) by VIRAL thymidine kinase (virus activates drug to it's toxic form);

Tx: HSV (simplex, fevere blisters, genital infx, encephalitis), VZV, CMV (esp in BM transplant pt); 

SE: HA, nausea, diarrhea, renal (Crystalline nephropathy + adjust dose in failure), CNS (tremors, delirium, seizures);

Anti-Herpes Drug - Nucleoside (Purine) analog;

Acyclovir prodrug;

Inhibits viral DNA polymerase by direct binding and by causing chain termination;

Req (+P) by VIRAL thymidine kinase (virus activates drug to it's toxic form);

Tx: HSV (simplex, fevere blisters, genital infx, encephalitis), VZV, CMV (esp in BM transplant pt); 

SE: HA, nausea, diarrhea, renal (Crystalline nephropathy + adjust dose in failure), CNS (tremors, delirium, seizures);

Anti-Herpes - Nucleoside analog;

Inhibits viral DNA polymerase by competitive inhibition only - No chain termination;

Penciclovir prodrug - guanine analog;

Req (+P) by VIRAL thymidine kinase;

Tx: HSV, VZV, CMV, also HBV;

SE: Well tolorated (HA/N/D);

Anti-Herpes Drug - Nucleoside (Purine) analog;

100x more potent than Acyclovir;

Inhibits viral DNA polymerase by direct binding and by causing chain termination;

Req (+P) by VIRAL thymidine kinase (virus activates drug to it's toxic form);

 Tx: DOC tx CMV/CMV Retinitis;

SE: Myelosuppression, Teratogenic, HA, N/D;

Anti-Herpes - Cytidine NucleoTIDE analog;

Does Not require (+P) by viral TK;

Tx: HSV/VZV (esp in Acyclovir resistant strains), CMV Retinitis (IV admin can delay the progression of CMV retinitis in HIV pts);

SE: Nephrotoxic, neutropenia, carcinogenic, ocular hypotony*, potential carcinogen*

Inorganic Pi analog - Non-Nucleoside Anti-Herpes agent;

Inhibits HSV DNA pol by binding to the Pi binding site and preventing cleavage and Inhibits HIV RT;

No (+P) required for activation;

Tx: Nucleoside resistant cases (HSV, VZV, CMV), CMV retinitis, HIV;

SE: Nephrotoxic*, N/V, anemia, fatigue

Anti-hepatitis C - nucleoside analog (G);

Interferes with GTP synthesis - competitive inhibitor of GTP 5' capping of viral mRNA;

Concentrates in RBCs;

Oral or aerosol admin;

Tx: HCV, RSV*;

SE: Dose-dep hemolytic anemia*, teratogenic (Cat X), BM suppression;

Aerosolized form well tolorated with mild irritation and possible pulm fxn decrease.

Anti-Parkinsonism, Anti-flu A - Uncoating inhibitor;

Blocks HA glycoprotein maturation - blocks binding to M2 ion channel, No internal acidification;

Works on Flu-A ONLY;

Enhances DA release;

"Good alternative to flu vaccine" in IC and elderly;

Resistance: via single aa mutation at the transmembrane region of M2;

SE: Restless, depression, psychosis, hallucinations, confusion;

CI: seizures, heart failure

Anti-flu A and B - Viral Release Inhibitor;

Inhibits viral neuraminidase - no cleavage of sialic acid - destroys receptors recognized by viral Hemagglutanin (HA) - no detachment from host cell - promotes viral aggreagation/↓ viral spread;

Admin via inhalation (low PO bioavail);

Tx: Flu-A(2nd line) and B;

Resistance via HA/neuraminidase mutations;

Typical Anti-Psychotic;

Inhibits D2 receptor (potency relates to D2 blocking strength) - effective for positive symptoms;

Aliphatic side chain - low potency (↓ risk of EPS, ↑ risk of anti-muscarinic effects);

Tx: Huntington's chorea (DA antagonism);

SE: Neuroleptic Malignant Syndrome (risk with all antipsychotics but greater with Chlorpro and Haldol)

SE: Corneal deposits, ↑ PRL (severe), ↓ insulin, Jaundice, Anti-diuretic effects*, orthstatic hypoT*, skin rxns, EPS, lowers seizure threshold*;

Typical Anti-Psychotic;

Inhibits D2 receptor (potency relates to D2 blocking strength) - effective for positive symptoms;

Piperdine ring - ↓ incidence of EPS*;

SE: ↑ PRL, highly anti-muscarinic;

Typical Anti-Psychotic;

Inhibits D2 receptor (potency relates to D2 blocking strength) - effective for positive symptoms;

Aliphatic side chain - High* potency;

Availible in Depot formation;

Tx: Huntington's chorea (DA antagonism), psychosis;

SE: EPS (lots dt strong D2 blocking, though less antimuscarinic effects), ↑ PRL, lowers seizure threshold*, Neuroleptic malignant syndrome*

Atypical Anti-Psychotic;

D2 (lower affinity and 5-HT2 (high affinity) antagonism;

↑e fficacy for Negative symptoms (as well as positives); Limited EPS;

SE: Blood dyscrasias (esp leukopenia), ↑ risk of DM typeII, Weight Gain*;

Atypical Anti-Psychotic;

D2 (low) and 5-HT2 (high affinity) antagonism;

↑ efficacy for Negative symptoms (as well as positives);

Tx: Psychosis in children and teens;

Limited EPS;

SE: ↑ PRL, ↑ risk of DM typeII, Moderate incidince of METABOLIC SYNDROME;

Atypical Anti-Psychotic;

D2 (less) and 5-HT2 (high affinity) antagonism;

↑ efficacy for Negative symptoms (as well as positives);

SE: Weight Gain, METABOLIC SYNDROME (highest incidence*), ↑ risk of DM type II;

Atypical Anti-Psychotic;

D2 (low) and 5-HT2 (high affinity) antagonism;

↑ efficacy for Negative symptoms (as well as positives); No effect on PRL levels*;

SE: Moderate incidence of METABOLIC SYNDROME, ↑ risk of DM type II;

Atypical Anti-Psychotic;

D2 (low) and 5-HT2A,1A,2C (high affinity) antagonism;

↑ efficacy for Negative symptoms (as well as positives); Limited EPS;

SE: ↑ risk of DM type II, low incidence of metabolic syndrome;

Atypical Anti-Psychotic;

D2 partial agonist (blocks full agonist binding), 5-HT2 antagonist, and 5-HT1A partial agonist;

↑ efficacy for Negative symptoms (as well as positives);

No effect on PRL levels;

SE: Lower incidence of SE dt MoA, ↑ risk of DM type II, low incidence of metabolic syndrome;

Cortex - ↓ seizure threshold;

Basal ganglia - ↑ DA metabolism, ↑ Ach turnover;

Limbic - main site of anti-psychotic efx;

Hypothalamus - ↑ PRL;

Brainstem - ↓ reflexes;

CTZ - protect against N/V*

Atypicals ↑ DM risk;

(Chlorpromazine additionally impairs glucose tolorance and increases insulin release);

Direct and indirect effects;

Orthostatic hypotension - esp chlorpromazine and throazidine*

Acute dystonia (muscle spasms);

Akathesia (ants in the pants);

Parkinsonian syndrome;

Neuroleptic Malignant Syndrome (high morality, fever, parkinsonis, tremor, ↑Crkinase, Myoglobinemia);

Perioral tremor (rabbit syndrome);

Tardive dyskinesia (stereotyped, tic-like movements)

Dry mouth;

Blurred vision; Constipation;

Nasal congestion;

Orthostatic hypoT

Parkinsonism Drug;

Crosses BBB and is conv to DA by endogenous L-AAD @ CNS and in periphery (↑ dose req'd in monotherapy);

Oral admin before meals: ↓ competition @ transporters;

Tx: First line for PD but can only use 3-5 years;

SE (mostly with monotherapy): anorexia/GI upset, orthostatic hypoT, arrhythmias (Afib), tachycardia;

Interactions: Vit B6 (which ↑ L-DOPA metabolism), MAOIs (HTN Crisis);

CI: Glaucoma, psychosis, PUD, CV dz, melanomas (?)

Parkinsonism Tx;

L-DOPA fxn PLUS... Peripheral inhibitor of L-AAD (the enzyme that converts L-DOPA to DOPA - ↓ dose of L-DOPA req for therapy;

Fluctuating responses;

SE: depression, anxiety, delusions, chorea, tics;

Interactions: Vit B6 (↑ metab of L-DOPA), MAOIs (HTNsive crisis);

CI: Glaucoma, psychosis, PUD, CV dz, melanoma (?)

Parkinsonism Drug - DA receptor agonist;

D2 agonist, D1 partial agonist;

Activation of D2 = ↓ activation of indirect basal ganglia pathways; 

Tx: EARLY Parkinson's dz (prefered, can be combo with L-DOPA in more advanced dz);

Selectivity reduces adverse SE/interactions;

Parkinsonism Tx - Cheap*;

D1 and D2 receptor agonist;

↑ effectiveness over bromocriptine;

Activates/agonizes D2 - activation of indirect basal ganglia pathways (allows prevention of unwanted mvmt);

Tx: Early PD, prolactinomas (inhibiton of PRL release);

Parkinsonism Drug - DA receptor agonist;

Activates D2 only - ↓ activation of indirect basal ganglia pathways;

D2 selective agonist, may also act as a free radical scavenger;

Tx: EARLY Parkinson's dz

Parkinsonism Tx - COMT inhibitor;

Prolongs the axn of L-DOPA and ↓ it's transport-competitor in GI/BBB 3OMD;

PERIPHERAL AXN;

Preferred due to lower SE than Tolcapone (which is not selective for the periphery);

Parkinsonism Drug - Anti-muscarinic;

Alters DA/Ach balance by blocking Ach-stimulation of striatum;

Tx: early Park or used as an adjunct to L-DOPA;

SE: drowsiness, inattention, delusions, hallucinations, typical ANS anti-Ach axns

Parkinsonism Drug - Anti-histamine/anti-muscarinic;

Alters DA/Ach balance by blocking Ach-stimulation of striatum;

Tx: early Park or used as an adjunct to L-DOPA;

SE: drowsiness, inattention, delusions, hallucinations, typical ANS anti-Ach axns

Alzheimer's Dz Tx;

Reversible Ach-esterase Inhibitor;

↑ lvls of Ach;

Long t1/2 - 70hrs;

Tx: Advanced AD

SE: GI, insomnia (Wild Dreams), bradycardia

Alzheimer's Dz Tx;

Reversible Ach-esterase Inhibitor;

↑ lvls of Ach;

Shorter half life, more renal handling;

SE: GI, insomnia, bradycardia

ALS tx;

↓ Glutamate (excitatory NT) release by (1) stablizing the inactive state in Na-channel, (2) blocking V-gated, activated Ca-channel, Also (3) blocks NMDA channel;

Met by CYP1A2;

High protein binding;

Reduces excitotoxicity and can prolong life by 2 months in ALS pts;

SE: fatigue, sedation, liver dz

MS tx - Anti-inflammatory;

Monoclonal Ab that restores BBB - ↓ immune response in the CNS of 67% of MS pts;

More effective than interferon;

Tx: MS and also Crohn's;

SE: PML!* (progressive multifocal leukoencephalopathy)

Anti-Epilepsy Drug - Hydantoin;

Stabilizes inactive state of Na channels (some inh of Ca2+ channels);

Met by CYP2C4, induces 2C and 3A*;

Zero Order Kinetics*;

Competes w/ warfarin, OCT, carbamazepine for protein binding sites;

Tx: 2nd line drug only (Partial/simple/complex, Tonic-clonic, or Status epilepticus);

SE: [narrow TI] nystagmus, ataxia, arrhythmias, coarsened face, hirsutism, gingival hyperplasia, peripheral neuropathy*, bone disruption, teratogenic*

Interactions: Competition with Valproate and Warfarin for protein binding, CYP induction ↓ [Carbamazepine] and of OCPs*

Anti-epilepsy Drug - barbiturate;

Prolongs duration of opening of GABA receptor Cl- channels. Blocks AMPA receptors;

Induce CYP2B6 and UGT;

Tx: Not 1st/2nd line AED dt sedation;

SE: Sedation*, lethargy, nystagmus, rash, megaloblastic anemia, ↓ vitD

Anti-epilepsy Drug and Mood-stabilizer;

Delays recovery of inactive state Na channels;

Met/activated by CYP2C9,3A4 to active 10,11-epoxide;

Induces CYP1A2, 2B6, 2C19, UGT;

Tx: DOC for simple/complex partial seizures and for generalized tonic clonic seizures, also tx bipolar* disorder, and trigeminal neuralgia*;

Tx depression typically assoc w/ Huntington's*;

SE: Blood dyscrasias (leukopenia), diplopia, ataxia, mild GI upset.

Anti-epilepsy Drug;

Inhibits the low threshold T-type Ca current in thalamic neurons - prevents 3Hz spike/waves;

↑ AUC when given w/ valproic acid*;

Met by hydroxylation;

Tx: DOC for absence seizures;

SE: [tolerance] euphoria, hiccups*, fatigue

Anti-epileptic Drug;

Stabalizes inactive Na channels, ↑ Ca current, stimulates GABA synthesis and inhibits degradation;

Met by UGT via beta-ox - also inhibits it;

Inhibits CYP2C9;

Tx: DoC for Atypical Absence, myoclonic, and atonic eizures, also tx absence, TC and partial as 2nd line;

↑ [plasma] phenobarbital, phenytoin, carbamazepine;

SE: heartburn, liver toxicity, teratogenic*;

Anti-epilepsy Drug - BNZ;

↑ opening of GABA Cl channel;

Can be given rectally or IV;

Tx: refractory myoclonic, atonic, absence;

SE: sedation, lethargy

Anti-epilepsy Drug- BNZ;

↑ probability of opening of GABA Cl channel;

IV or rectal admin;

Tx: DOC status epilepticus;

SE: sedation, lethargy

Anti-epilepsy Drug - BNZ;

↑ probability opening of GABA Cl channel;

Long acting*, can admin rectally;

Tx: 2nd line for status epilepticus;

SE: sedation, lethargy

Anti-epileptic Drug;

Inhibits Na channels, may also reduce T-type Ca channel current;

Tx: adjunct for parital seizures, infantile spasm, myoclonic, generalized and absence;

Met by CYP3A4 (use with phenobarbital, phenytoin, or carbamazepine will accelerate breadown of this drug);

Muscle Relaxant;

GABA(B) agonist - inhibitory and hyperpolarizing. Inhibits substance P;

Admin oral or intrathecal;

Don't d/c abruptly - rebound neural hyperactivity;

Tx: Spasticity, MS, muscle spasm, spinal cord trauma;

SE: Sedation,

Additive Effects: CNS depression, hypoT, and hypoglycemic (watch with antidiabetic agents)

Muscle Relaxant;

Pre-synaptic alpha2 agonist - ↓ axn of spinal motor neurons;

Admin oral - high first pass met.;

Tx: spasticity, MS;

SE: SEDATION, hepatotox, anticholinergics, hypoT;

Additive Effects:CNS depressants, Hypotensive agents;

CI: with other drugs acting on alpha2;

Muscle Relaxant;

Blocks Ryanodine receptor on the SR of muscle cells- confine Ca in the SR - ↓ sk muscle response to stim;

Admin oral or IV;

Hepatic met (perform liver fxn tests);

Tx: Spasticity, MS, malignant hyperthermia, neuroleptic malignant syndrome;

SE: phlebitis, Heptotoxic w/ estrogens*, CNS depression, floppy baby syndrome (crosses the placenta);

Interactions: CNS depressants, CV collapse with CCBs, hepatic tox with estrogens;

Muscle Relaxant;

General CNS/SC depression to sedate and ↓ pain, no direct efx on conduction;

Met by CYP2C19*;

Tx: Muscle spasms;

SE: sedation, insomnia, vertigo, ataxia, vision loss, mydriasis, orthostatic hypoT;

Additive Effects: CNS depressants, CYP inhib/inducers, Anticholinergics*

Muscle Relaxant-ish;

GABA drug, binds to the alpha-2-delta component of GABA-R to ↓ neuronal Ca channel currents;

↓ neuropathic pain and anxiety;

Tx: Fibromyalgia (muscle/joint pain);

SE: Sedation, blurred vision, weight gain*, swelling of the hands and feet*, xerostomia;

Additive CNS depression

Anti-Microbial -cell wall synth-Narrow Spec - B-lactam;

The Oral "Natural Pen";

Blocks cell wall-synth enzymes;

Oral admin, Glomerular filtration, secretion;

Tx: G+ cocci and bacilli (staph, strep), some G- cocci, GC, spirochetes (T. pallidum); 

SE: Hypersensitivity* (>2d = delayed, acute =more severe), N/V/D, rash, neurotoxic

Anti-Microbial - cell wall synthesis;

Penicillinase Resistant B-lactam;

Blocks cell wall-synth enzymes;

Parenteral admin, Glomerular filtration, secretion;

SE: rash, neurotoxic;

No longer on the market, was the original Penicillinase resistant beta lactam abx;

Anti-Microbial - cell wall synthesis;

Penicillinase Resistant B-lactam - "Anti-staph";

Blocks the action of transpeptidases (PBPs) in synthesizing bacterial cell walls (cross linking PGs);

IM or IV admin;

Glomerular filtration, secretion - Highly protein bound;

Tx: B-lactamase-producing staph;

SE: decreases electrolytes*, rash, neurotoxic

Anti-Microbial - cell wall synthesis;

"Extended spectrum" beta lactam;

Blocks the action of transpeptidases (PBPs) in synthesizing bacterial cell walls (cross linking PGs); Glomerular filtration, secretion;

Req supplement after dialysis*;

Tx: [G+ and G- rods/bacilli] H. flu, E. coli;

Resistance: B-lactamase (G-);

SE: Delayed Rash*, Diarrhea, Pseudomembranous Colitis*, neurotoxic*

Anti-Microbial - cell wall synthesis;

B-lactam - "Extended spectrum";

Blocks the action of transpeptidases (PBPs) in synthesizing bacterial cell walls (cross linking PGs);

Oral admin;

Glomerular filtration, secretion - Req supplement after dialysis*;

Tx: [G+ and G- rods/bacilli] H. flu, E. coli;

Resistance: B-lactamase* (G-);

SE: Delayed Rash*, Pseudomembranous colitis*, neurotoxic*

Anti-Microbial - cell wall synthesis -1st Gen Ceph;

Renal tubular secretion - ↑ [plasma] w/ probenecid;

Tx: G+ cocci, many G- bacilli (think ampicillin);

SE: hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections;

Anti-Microbial - cell wall synthesis - 2nd Gen Ceph;

Renal tubular secretion - ↑ [plasma] w/ probenecid;

Tx: Less G+, more G- (H. flu, B. fragilis);

SE: hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections;

Anti-Microbial - cell wall synthesis - 3rd Gen Ceph;

Renal tubular secretion - ↑ [plasma] w/ probenecid; Highly metabolized PENETRATES CSF;

Tx: [severe] enteric G-'s, B. fragilis, H. flu, Pseudo.;

SE: Enterobacter Superinfections, hypersensitivity, phlebitis, IM pain, nephrotoxic;

Anti-Microbial - cell wall synthesis - 3rd Gen Ceph;

Renal tubular secretion - ↑ [plasma] w/ probenecid; Longest t1/2;

Does not require supplementation in dialysis;

  PENETRATES CSF;

Tx: [severe] enteric G-'s (B. fragilis, H. flu), Pseudomonas;

SE: ENTEROBACTER SUPERINFECTIONS, hypersensitivity, phlebitis, IM pain, nephrotoxic;

Anti-Microbial - cell wall synthesis - 4th Gen Ceph;

Renal tubular secretion - ↑ [plasma] w/ probenecid;

BROAD SPECTRUM - incl G+ B-lactamase producers;

Tx: Pseudomonas, Klebsiella, E.coli;

SE: hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections;

Anti-Microbial - cell wall synthesis - glycoprotein;

D-Ala-D-Ala binding;

BacteiroCidal effects w/ narrow spectrum;

Oral admin for mild GI infx, parenteral for systemic; Enters inflamm meninginges/CSF;

Resistance: Plasmid-mediated alteration in binding site;

Tx: DOC for MRSA, strep, enterococci,

2nd line for C. diff;

SE: Synergistic nephtrotox, ototoxicity (w/ loop diuretics), Red Man Syndrome*, ↓ [plasma] in multiple myeloma, GI, phlebitis

Anti-Microbial - Inhibits 50S ribosome;

Oral admin (100% bioavail), also parenteral;

Requ supplementation after dialysis;

Resistance: Pt mutations of 23s ribosome binding site;

Tx: VRE (E. faecium and faecalis)[static], MRSA [static], Strep [cidal] - reserve for serious infx;

SE: N/V, diarrhea, pseudomembranous colitis*, inhibits MAO non-selectively (Caution in co-admin w pseudoephedrine, SSRIs, tyramine etc...);

CI: PKU

Anti-Microbial - 30S ribosome - Tetracycline;

Passive diffusion thru porin channels into cell - reversible 30S ribosome binding;

Abs (best in acidic stomach stomach) inhibited by multivalent cations;

Crosses placenta, enters milk;

Resisitance: slow, via ↓ influx & ↑ efflux - Resistance to one Tetracycline = Resistance to all*;

Tx: [BROAD] - Mycoplasma*, Chlamydia, Rickettsae*, Spirochetes, protozoa, lyme, acne, peridontal dz;

SE: Hepatotoxic*, Photosensitivity, Tooth discoloration, (LESS) GI, avitaminosis, vertigo, ↓ bone growth, Superinfections are common;

CI: Children <8 yrs, Pregnancy, w dairy products, antacids or supplements (divalent cations);

Anti-Microbial - 50S ribosome (irreversibly) - Macrolide;

STATIC axn - Narrow Spectrum;

Oral admin - Short t_1/2;

Resistance: [cross-res w/ Clinda*] - rapid - plasmid-mediated ↓ influx, target altered, and drug hydrolysis;

Tx: [G+] DOC for Legionaire's Dz*, Pneumociocci, GAS, Listeria, Corynebacterium, Lyme Dz;

SE: Inhibits CYP450, Cholestatic Hepatitis*, can prolong QT interval

Anti-Microbial - 50S ribosome (irreversibly) - Macrolide;

STATIC axn - Narrow Spectrum;

Oral admin (↓ GI fx, ↑ acid stability);

Resistance: [cross-res w/ Clinda*] - rapid - plasmid-mediated ↓ influx, target altered, and drug hydrolysis;

 Tx: [G+] Erythro's plus MAC'S DOC, H.flu, strep, H.pylori, Ct, Moraxella;

SE: Inhibits CYP450, Cholestatic Hepatitis*

 Anti-Microbial - 50S ribosome (irreversibly)- Macrolide;

STATIC axn - Narrow Spectrum;

Oral admin (Long t_1/2);

Resistance: [cross-res w/ Clinda*] - rapid - plasmid-mediated ↓ influx, target altered, and drug hydrolysis;

 Tx: [G+] DOC for Legionaire's/MAC/Campylobacter*, H.flu, strep, H.pylori, Ct, Lyme Dz;

SE: Inhibits CYP450, Cholestatic Hepatitis*

Anti-Microbial - 50S ribosome - Ketolide;

Sim.to macrolides - irreversible 50S ribosome inhibition;

Penetrates bone, not CSF*;

Acid stable, slow resistance;

Tx: Anerobes (B. Fragils), G+, toxo, P. jiroveci;

SE: Pseudomembranous Colitis**, GI, rash

Anti-Microbial - 30s ribosome (irrev. dmg) - AMG;

E-dependant (ETC and O2 req) diffusion through outer porin channel;

Conc-dependent killing - use bolus dose (parenteral);

Enters inflamm meninges/CSF, renal cortex, inner ear;

Limited cross-res within class;

Tx: [severe aerobic G-] enterococcus endocarditis, MRSA, staph epi;

SE: Ototoxicity (irrev.), Nephrotox (PCT, renal cortex), neuromuscluar blockade, teratogen*

Anti-Microbial - 30s ribosome (irrev. dmg) - AMG;

E-dependant (ETC and O2 req) diffusion through outer porin channel;

Conc-dependent killing - use bolus dose (parenteral);

Enters inflamm meninges/CSF, renal cortex, inner ear;

Limited cross-res within class;

Tx: [severe aerobic G-] enterococcus endocarditis, MRSA, staph epi;

SE: Ototoxicity (irrev.), Nephrotox (PCT, renal cortex), neuromuscluar blockade, teratogen*

Anti-Microbial - 30s ribosome (irrev. dmg) - AMG;

E-dependant (ETC and O2 req) diffusion through outer porin channel;

Conc-dependent killing - use bolus dose (parenteral);

Enters inflamm meninges/CSF, renal cortex, inner ear;

Limited cross-res within class;

Tx: [severe aerobic G-] enterococcus endocarditis, MRSA, staph epi;

SE: Ototoxicity (irrev.), Nephrotox (PCT, renal cortex), neuromuscluar blockade, teratogen*

Anti-Microbial - Folic acid metabolism;

Selective inhibition of bacterial DHFR - prevents reduction of di- to tetra-hydrofolate (blocks de novo thymine synthesis and therefore blocks DNA synthesis);

IV or Oral

(Alone, oral admin can be used as prophy or tx for uncomplicated UTI - MC combined as TMP-SMX)

Penetrates CSF, prostate, vaginal fluid*;

Resistance: altered DHFR affinity;

SE: Disulfram-like rxn, Thrombocytopenia due to folate depletion;
Relatively CI in pregnancy

Anti-Microbial - DNA gyrase - 2nd gen fluoroquinolone; 

↓ abs w/ multivalent cations in antacids;

Inhibits CYP450;

Resistance: ↓ porin proteins, efflux, or binding site axn;

Tx: UTI/GIT infx, G- systemic axn vs aerobes (HLP) and enterics (E.coli, Kleb, Moraxella), intracellular (accumulates in macs/leukocytes - Chlym, legionella), GC, mycobacterium, best for pseudomonas;

SE: GI, dizzy, photosensitivity, seizures*, crystalluria*;

CI: Pregnancy, youth

Anti-Microbial - DNA gyrase - 2nd gen fluoroquinolone; 

↓ abs w/ multivalent cations in antacids;

Inhibits CYP450;

Resistance: ↓ porin proteins, efflux, or binding site axn;

Tx: Improved G+ axn, Broad G-, Intracellular bacteria;

SE: GI, dizzy, photosensitivity, seizures*, crystalluria*, only 3rd gen fluro that does not cause QT prolongation;

CI: Pregnancy, youth

Polyene Antifungal - cell membrane;

Binds ergosterol, forms pore - allows leakage of K, Mg - FungaCidal efx;

IV admin - high binding to beta-lipoprotein;

Resistance: in Candida;

Tx: [deep, systemic fungal infx, ok in pregnant women] Candida, Crypto, Aspergillus, Blasto;

SE: Nephrotoxic**, fever, thrombophlebitis, hypersensitivity, shock/hypoT*;

Antifungal;

Prodrug-inhibits thymidylate synthase =inhib DNA synth;

Cidal/static dep. on dose and organism;

Oral admin - Virtually always given with AmphB*;

Penetrates the CSF*

↓ dose in renal failure and when given w/ AmpB;

Resistance: ↓ permease, ↓ cytosine deaminase (fail to activate the drug);

Tx: [systemic mycoses] Candida meningitis;

SE: Hematological tox (can be letha, dose-dep), Colitis

Antifungal - cell membrane - Azole;

Inhibits ergosterol synthesis;

Severe CYP450 inhibition;

Resistance: rapid if used alone;

Tx: [broad] Invasive Aspergillus, Scedosporium, Fusarium;

SE: Visual Disturbances (Color) + Photosensitivity (V for Visual disturbances)*, Hepatotoxic, Teratogenic;

Antifungal - Cell membrane;

Inhibits ergosterol synthesis;

Mild CYP450 inhbitor;

Resistance is rapid if used alone;

Tx: [broad] yeasts, dermatophytes, systemic mycoses, adjunct in Cushings (CYP inhibition of cortisol synth);

SE: ↓ testosterone and prevent adrenal steroidogenesis** (gynecomastia, reduced libido etc...), Teratogenic

Antifungal;

Inhibits squalene epoxidase - inhibits ergosterol synth;

Highly protein bound -Concentrates in keratin -hair/nails;

Oral or Topical admin;

Tx: Onychomyosal fungal infxns - nails;

SE: HA, GI, Taste Changes*, Cholestatic Hepatitis*

Antifungal;

FungaStatic* - disrupts fungal mitotic spindle;

Conc in keratin precursor cells via active transport;

CYP450 inducer;

Tx: Dermatophytes (edermophytan, microsporum, trichophytan);

SE: HA, GI, Photosensitivity;

Anti-mycobacterium - Cell Wall;

Blocks mycolic acid synthesis;

Cidal if rapid growth/ static if slow;

Oral admin;

Enters inflamm meninges/CSF, placenta, breastmilk;

↓ efx w/ anatacids, steroids - Met by acetylation;

Resistance is rapid, use in combo;

Tx: First Line for TB;

SE: Perhiperal Neuropathy, Hepatotoxic, B6 deficiency* (supplement Pyrodoxal Phosphate, PLP)

Anti-mycobacterium - RNA Pol;

Binds beta subunit of RNApol - Cidal to intra and extracellular mycobacteria;

Oral admin - Enters CSF*;

CYP450 inducer;

↑ lvls if take w/ probenecid;

Tx: TB (1st line), MRSA, mengingococcus, anti-leprosy*;

SE: Red/orange fluids, GI, fever/chills/aches, hepatotoxic (jaundice)

Anti-mycobacterial;

Oral admin - ↓ abs w/ antacids (Al+++);

BacterioStatic;

Enters placenta, breastmilk, inflamed meninges/CSF;

Slow resistance;

Tx: First Line TB and MAC;

SE: Optic neuritis, hyperuricemia*, allergic rxns

Herbal supplement - Natural coumarin derivative;

Interaxn w/ Rx anticoagulants

Herbal supplement;

Contains synephrine, an alpha-1 agonist*;

Inhibits CYP3A4;

SE: stroke, angina, ischemic colitis

Dietary supplement;

Potent antioxidant;

'Tx': Good Evidence: HTN, ischemic heart disease, prevention of statin-induced myopathy;

SE: Generally well tolorated but poss warfarin interaxn due to VitK-like structure

Dietary Supplement;

'Tx' to give an Immune boost - no supporting evidence; Thus antagonizes immunosuppressants;

Induces CYP3A4; Inhibits CYP1A2 and intestinal 3A4; Lots of Interactions without clear evidence of effects.

Herbal supplement;

'Tx' (decent evidence): Reduces cholesterol;

SE: antiplatelet & prolonged bleeding*

Herbal supplement;

'Tx': Prevention of Alzheimers Dz;

SE - anti-platelet, Inh CYP1A2 and 2D6

Herbal supplement;

MAY provide Immune boost, CV benefits, lower LDL, decrease [glucose], boost response to flu vaccine;

Thus antagonizes immunosuppressants*;

Other SE: prolonged bleeding, inhibits CYP2D6

Herbal supplement - natural coumarin derivative; Interaxn w/ Rx anticoagulants;

Estrogen-like axns - increase risk of cancer of the lining of the uterus/breast cancers (?)

Herbal supplement;

'Tx' as a laxative;

SE: hepatotoxic and carcinogenic*

Herbal supplement;

'Tx': depression (good evidence);

Induces CYP3A4, 1A2, 2C9

Mineral supplement;

Key cofactor in enzymes, protein and carb metabolism; 

Reduces childhood diarrhea in developing countries helps heal gastric ulcers;

Tx: Sickle cell, acne, ADHD, Down's, herpes, high cholesterol, plaques and gingivitis

Hematopoietic Growth Factor;

Acts on progenitor cell receptor to increase RBC production (BFU-E and CFU-E);

IV or SC admin;

Tx: Anemia assoc w/ AIDS, chemo, preemies, chronic inflamm dz's, renal failure;

SE: cardiotoxic, nephrotoxic*

Myeloid Growth Factor;

Stimulates myelopoiesis of granulocytes, etc.;

Tx: severe neutropenia;

SE: granulocyte spike, bone pain, rash

Myeloid Growth Factor;

Stimulates myelopoiesis of granulocytes, etc.;

Tx: severe neutropenia (AIDS pt on Zidovudine);

SE: granulocyte spike, bone pain, rash

Megakaryocyte Growth Factor;

Recombinant IL-11 which stimulates lymphoid and myeloid growth;

Tx: Thrombocytopenia;

SE: fatigue, dizzy, dyspnea, arrhhythmia, edema

Mineral Iron;

Oral admin;

Tx: DOC for iron deficiency anemia*;

SE: heartburn, nausea, GI

Vitamin;

Admin parenteral > oral;

Tx: B12 deficiency (megaloblastic - pernicious anemia)

Vitamin;

Oral or parenteral admin;

Use before preg thru breasfeeding;

Tx: specific deficiency (think prego, chemo, chronic EtOH, upper intestine dz);

Counteracts AED's* (Phenobarbital, phenytoin)

CNS stimulant;

Indirect dopamine agonist - ↑ BP, wakefulness, alertness, concentration, self-confidence, euphoria, physical performance, wt loss (though tolorance develops to app suppressant effects);

Psychological dependence (abuse liability);

Tx: Obesity, narcolepsy, ADHD;

SE: arrhythmias, angina, HA, abuse (DA reward), neurotoxic, convulsions, cerebral hemorrhage, schizophrenogenic*

CNS stimulant;

Indirect dopamine agonist;

↑ BP, wakefulness, alertness, concentration, self-confidence, euphoria, physical perform, wt loss;

Psychological dependence - abuse potential;

Tx: Obesity, narcolepsy, ADHD;

SE: arrhythmias, angina, HA, abuse (DA reward), neurotoxic, convulsions, cerebral hemorrhage, schizophrenia.

CNS stimulant [Concerta] -mild;

Indirect dopamine agonist;

↑ BP, wakefulness, alertness, concentration, self-confidence, euphoria, physical perform, wt loss;

Still has abuse potential;

Tx: Narcolepsy, ADHD;

SE: arrhythmias, angina, HA, abuse (DA reward), neurotoxic, convulsions, cerebral hemorrhage, schizophrenia*

'Stimulant' (not an effective stimulant);

NE reuptake inhibitor;

Tx: ADHD (esp approved to tx adults);

Low abuse potential (consider in abuse prone teens);

SE: Anorexia/appetite suppression, insomnia, ↑ HR/BP

Stimulant;

DA, NE, serotonin reuptake inhibitor;

Tx: Short-term for obesity (Don't exceed<6 mo. use);

SE: Serotonin syndrome*, HTN;

CI: MAOI, anorexia, HTN, hypersensitivity;

Stimulant;

Mechanism unknown - No DA effect - No abuse potential;

Tx: Narcolepsy;

Induces CYP450*;

SE: HA for 1 week

Stimulant;

Indirect NE and serotonin agonist;

Tx: short term for obesity;

Low abuse potential;

CI: atherosclerosis, HTN, hyperthyroidism, hypersensitivity to sympathetic amines, CV dz, MAOIs

Anticoagulant - Arterial and Venous thrombosis inhibition;

Activates ATIII to inactivate thrombin and factors IX, X, XI, and XII;

Admin SQ or IV;

Rapid Onset, Variable t_1/2/binding to plasma proteins; -

Monitor PTT;

Works only for soluble thrombin;

SE: HIT (at 5-10 days) dt formation of Heparin-PF4 complexes and LT activation - thrombocytopenia and clotting*;

Low MW Heparin;

Admin SQ;

Small molecule, long t_1/2;

↑ anti-Xa axn, ↓ plasma protein binding, ↓ anti PLT axn;

No need to monitor;

Tx: DVT prophylaxis;

SE: less potential for HIT (at 5-10 days, though still possible)

Direct Thrombin Inhibitor;

Irreversibly binds active site and exosite 1 of Thrombin;

Acts on soluble and Clot-bound thrombin;

No immune-med thrombocytopenia;

Source - leech saliva;

Tx: HIT;

SE: (less) hemorrhage;

CI: renal failure

Direct Thrombin Inhibitor;

Irreversibly binds active site and exosite 1 of thrombin; Acts on soluble and Clot-bound;

No immune-med thrombocytopenia;

Source - recombinant form of Hirudin;

Tx: HIT;

SE: (less) hemorrhage;

CI: renal failure

VitK Antagonist;

Competes w/ Vitamin K  for binding of epoxide reductase - ↓ vit K - Blocks synthesis of factors II, VII, IX, X - ↓ thrombin formation;

Slow onset (36-72 hrs), long duration - monitor PT;

Tx: DVT, PE, Afib, Rheumatic heart dz (DOC for first 3);

SE: Skin necrosis (protein C def), hemorrhage, transient pro-coagulant (inh Protein C), drug interactions (incl. EtOH);

CI: Liver disease

Non-selective COX1/2 irreversible Inhibitor - anti-PLT;

Acetylation of enzyme;

COX1 inhibition - no TXA2 - ↓ aggregation. COX2 inhibition - no PGI2 - ↑ aggregation;

Tx: CHD; SE - GI bleed, hemorrhagic stroke, asthma;

CI: Coumarin, PUD, asprin hypersensitivity (asthma);

Max dose <4g/day

Phosphodiesterase (PDE) Inhibitor - anti-platelet;

↑ cAMP - inhibits aggregation (enhanced prostacyclin-mediated axn) and ↑ adenylate cyclase (↓ adenosine);

Vasodilator;

Tx: Not used alone - adjunct of aspirin for anti-platelet, adjunct w/ warfarin for thrombosis prevention in pt with prosthetic valves, used to Induce Coronary Steal*;

SE: HA, dizzy, GI, Coronary Steal*

GP IIb/IIIa Receptor Blocker - anti-platelet;

Monoclonal Ab that targets the GP IIb/IIIa receptor;

IV admin;

Tx: Given before/during cardiac cath and angioplasty;

Helps restore blood flow in failed rescue angioplastys*

Dramamine;

1st Gen antihistamine;

Sedative, anti-emetic, GI cramps, anticholinergic;

Tx: Allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);

SE: Disorientation/delirium,  sedation, dystonia, nasal congestion;

CI: Asthma and glaucoma

Antitussive - cough suppression;

Opiate derivative but non-narcotic;

No analgesia;

Met at CYP2D6;

Acts on non-opioid receptors;

SE: hallicinogen, dry mouth, tachycardia, disorientation, depersonalization, somnolence

Insectiside - parasympathomimetic;

Irreversible Anticholinesterase;

Tx: resistant scabies and pediculosis;

Remember: acetylcholinesterase inhibitor (insecticide);

SE: systemic ingestion=cholinergic effects

Benzodiazepine - balanced anesthesia;

↑ activity of GABA receptor/channel;

Death from OD more diff than with barbs;

No analgesia;

Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects, wide safety margin;

(Flumazenil = specific BZ antagonist)

Aminoglycoside Antibiotic;

Topical, Oral, Enema;

Give enema to reduce colonic bacteria;

Tx: portal HTN, encephalopathy;

SE: Ototoxic, nephrotoxic, Teratogenic

Anticholinergic;

Sedation and amnesia;

Pre-op ancillary agent for anesthesia;

Tx: reflex bradycardia, blockage muscarinic anticholinesterases (NM blocker OD), Drying of secretions;

Blocks pathways from inner ear - Tx motion sickness

Beta-1 and 2 antagonist;

Direct effect on Na channels, anti-arrythmias;

Tx HTN, esp with CHF or prev MI;

SE see BB SEs

Intermediate acting insulin preparation;

Taken twice daily, lower peak and longer duration of action allows morning and evening dosing and prevents nocturnal hypoglycemia.

Anticoagulant - Direct Throbin Inhibitor;

Reversible binding;

Tx: Prophy for HIT for pt prone to it;

SE: Bleeding (lower risk dt specific activity)

Secreted by the D cells of the pancreas and by the paraventricular hypothalamus;

Inhibits the release of TSH and GH from the pituitary and Insulin and Glucagon from the pancreas* (4);

Short t_1/2;

Tx: Acromegly/Giantism, Glucogonomas, Insulinomas;

D2 Receptor agonist;

Higher affinity and longer half life than Pergolide;

Tx: Prolactinomas

Anti-Malarial drug;

Used in combination to treat fulpicarium in kids, adults, and pregnant women;

NOT AVAILIBLE IN THE US, only availible in the UK on a per pt basis;

Always give in combo to avoid resistance development;

Inhibitor of Oxytocin and ADH release from the posterior pituitary;

IV admin;

Tx: Used as a labor suppressant;

Study showed no better effects than placebo...but I guess we needed a 249th drug so this one is on the list.

Stimulant Laxative (promote evaculation of the colon);

Works directly on the large intestine to promote motility - stimulates enteric nerves to cause colonic mass mvmt;

Also a contact laxative; 

↑ fluid and NaCl secretion;

A toxic gas (colorless, odorless, tasteless, and initially non-irritating, difficult to detect). Produced in domestic or industrial settings by older motor vehicles and other gasoline-powered tools, heaters, and cooking equipment.

Sx of mild acute poisoning include lightheadedness, confusion, HA, vertigo, flu-like sx. Larger exposures can lead to significant CNS and cardio toxicity and death;

Causes adverse effects in humans by combining with Hb to form carboxy Hb (HbCO) which prevents O2 binding to Hb, ↓ the O2-carrying capacity of the blood = Hypoxia;

Tx: 100% O2 + hyperbaric O2 - which inc removal of CO from Hb^.

More potent testosterone derivative;

Generated from Testosterone via the actions of alpha-5 reductase (5% of testosterone undergoes 5α-reduction to form the more potent androgen);

During embryogenesis DHT has an essential role in the formation of the male ext genitalia, while in the adult DHT acts as the primary androgen in the prostate and in hair follicles^*

Congenital 5-alpha-reductase def causes pseudohermaphrodism (DHT is key in development of secondary sex charactaristics);

DHT cannot be converted by aromatase to estradiol*;

DHT is the primary contributing factor in male pattern bladness; 

Also plays a role in BPH and Prostate cancer by enlarging the prostate gland (blockage of 5 alpha reductase used to tx)^;

aka EDTA;

Is a hexadentate ("six-toothed") ligand and chelating agent (cans equester metal ions such as Ca²⁺ and Fe³⁺). After being bound by EDTA, metal ions remain in solution but exhibit diminished reactivity.

Tx: Mercury and Lead poisoning;

Antidote in methanol or ethylene glycol poisoning - used alone or in combination with hemodialysis;

Competitive inhibitor of alcohol dehydrogenase the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.

Ethylene glycol to oxylate and glycolate (metabolic acidosis and renal damage) and Methanol to formaldahyde and formic acid (metabolic acidosis and visual disturbances);

IV admin;

Anti-epileptic Drug;

Strucutral analog of GABA + may ↑ GABA release;

Tx: Adjunct for partial seizres, neuropathic pain tx, and neuralgia;

SE: are mild, somnolence, dizziness, ataxia, generally resolve;

Injectible GnRH;

Daily SQ admin;

Blocks the action of GnRH upon the pituitary = suppression of production/axn of FSH and LH;

Used to control ovulation (in assistive reproduction)

Semi-synthetic opioid (stronger than codine but much less powerful than morphine);

Narcotic analgesic and antitussive agent;

Oral admin;

Tx: Pain and cough;

SE: N/V, dizziness, drowsiness, respiratory depression;

CI with alcohol, cocaine, amphetamines, BNZ, barbituates;

Broad spectrum antiparacitic - anti-helminth/arthropod;

↑ Excitatory Glu channel permiability to Cl - causes hyperpolarization and paralysis of worms/mites;

Tx: Worms (esp in the tx of Oncherciasis in attempts to erradicate river blindness), but also effective against other worms (strogyloides) and mites/scabes;

SE: CNS depression possible;

Anti-Epileptic drug (AED);

MoA Unknown - binds to a synaptic vesicle protein,believed to impede nerve conduction across synapse;

Tx: Partial seizures, adjunct for general, partial, tonic-clonic seizures;

SE: Generally well tolorated - Fatigue, weakness, forgetfulness, occasionally depression/suicidal ideation

Vitamin B3, Niacin;

Essential nutrient;

Deficiency causes Pellagra (diarrhea, dermatitis, Dilated cardiomyopathy, dementia, and death)

[Prilosec]

Proton Pump Inhibitor;

Tx: PUD, GERD, dyspepsia, ZE syndrome and with Abx to tx H. pylori infx;

SE: HA, diarrhea, ab pain, nausea, dizziness, trouble awakening/sleep deprivation

Alli - Weight Loss agent;

Inhibitor of gastric and pancreatic lipases - blocks breakdown of ingested fats which makes them unabsorbable - eliminated;

Eating a fatty diet is associated with unpleasant side effects - aversion therapy, pt should limit fat intake;

SE: Steatorrea, flatulence;

CI: With cephalosporin (reduces its effectiveness)

Anticholinergic;

Competitive antagonist of M1,2 and 3 subtypes of the mAch receptor;

Tx: Urinary and bladder difficulties (frequency/incontinence by decreasing muscle spasms of the bladder - remember that parasympathetics trigger voiding - blocking them reduces frequency), hyperhydrosis (excess sweating);

SE: Dry mouth, constapation, blurred vision, drowsiness;

From the posterior pituitary;

Promotes milk let down and used in the induction of labor;

DA and NE reuptake inhibitor;

Highly hepatotoxic*

Schedule IV;

No longer availible generally in the US - shocker

• Can be used emergency tx for hyperthyroidism/thyroid storm (high amts of I  suppress secretion of thyroxine from the thyroid)

• Has been used topically to tx sporotrichosis.

• Symptomatic tx of erythema nodosum
• Thyroid protection during medical tx - admin non-radioactive potassium iodide prior to nuclear medicine scans to ensure that iodide from these radiopharmaceuticals is not sequestered by the normal affinity of the thryoid for iodide.
• Protection of the thyroid from radioactive fall out. Protective effect of KI lasts approximately 24 hours.

Vitamin B6;

Supplement in pt taking INH for TB tx;

Ultra-long-lasting sulfonamide used in combo with pyrithamine to tx/prevent malaria;

Avail. as gonadorelin hydrochloride;

IV admin via an infusion pump system;

Tx: induce ovulation in patients with hypothalamic hypogonadism;

Analog Leuprolide is used for continuous infusion, to tx breast carcinoma, endometriosis, prostate carcinoma, and precocious puberty;

T₄

Involved in controlling the rate of metabolic processes in the body and influencing physical development;

A prohormone and a reservoir for the active (T₃), which is about four times more potent.

T₄ is converted in the tissues by deiodinases incl thyroid hormone iodine peroxidase (TPO), to T₃.

Anti-PLT drug - GPIIb/IIIa inhibitor;

Synthetic/non-peptide;

IV admin;

Tx: w Heparin and asprin in pt with unstable angina, non-Q wave MI,and pt undergoing angioplastyto prevent ischemic events;

SE: Bleeding (incl intracranial bleeding);

Caution: bleeding conditions, CVD, older pt, HTN, pericarditis.

Antipsychotic and Anti-emetic;

SE: (Has higher risk for side effects than many other antipsychotics- it is not gold standard in antiemetic therapy) - Akathesia, tarditive dyskinesia, Neuroleptic Malignant Syndrome;

DDAVP;

Synthetic vasopressin;
Binds the V2 receptors on the collecting ducts inducing resorption of water (only);

Tx: Diabetes insipidus, nocturia (bedwetting);

SE: HA, flushing, hyponatremia, seizures*

Very effective delivery system for nicotine;
Delivered in bolus throughout the day. Reaches brain w/in 10 seconds. Addiction is to the rapid high brain concentrations achieved from smoking;

Nicotine itself is not carcinogenic, it is the 4,000 chemicals in cig smoke (aldehydes, polycyclic aromatic hydrocarbons, heavy metals) that are highly carcinogenic.

t1/2 = 2 hrs (chain smokers);

Women have a harder time quitting;

Smoking is more common in psychiatric populations (esp schzophrenics);

The highest dependence of any drug of abuse;