Term
|
Definition
Acts on target tissues (esp liver) through JAK2 (a TK) to initiated signalling pathways;
Production of IGF-1(&2) to exert effects;
Dec insulin sens, inc lipolysis, inc protein synth, inc epiphyseal growth;
Secretion stimulated by hypoglycemia, insulin;
Physiologic pulsatile release |
|
|
Term
|
Definition
hGH;
Replacement therapy in children;
Tx child - pituitary dwarfism (d/c when growth stops);
Tx adults - CV dz mortality, AIDS-associated wasting;
SE child (fewer) - leukemia, inc ICP, nausea;
SE adult - carpal tunnel, peripheral edema, arthralgia, myalgia;
CI - leukemia tx |
|
|
Term
|
Definition
D2 receptor agonist;
Dec prolactin production @ ant. pituitary;
Inc affinity, inc t1/2;
Tx hyperprolactinemia from pit. adenoma |
|
|
Term
|
Definition
Somatostatin analog - long acting;
Inh insulin, glucagon, GH, and TSH release;
Short t1/2;
Tx - insulinomas, glucagonomas, acromegaly, gigantism;
SE - diarrhea, nausea, abdominal pain |
|
|
Term
|
Definition
FSH + LH;
Extracted from post-menopausal urine;
IM admin;
Tx female infertility |
|
|
Term
| Gonadorelin hydrochloride (Factrel) |
|
Definition
Synthetic GnRH;
SHORT t1/2;
Diagnostic testing to diff pituitary and hypothalamic lesions in pts w/ hypogonadotropism |
|
|
Term
|
Definition
GnRH analog;
Inc t1/2, inc receptor binding - induces receptor downregulation;
Tx prostate cancer, uterine fibroids |
|
|
Term
|
Definition
Synthetic ACTH (24 AA);
Preferred to natural product b/c no vasopressin activity;
Use - test integrity of HPA axis |
|
|
Term
|
Definition
Produced in adrenal cortex (10mg/day);
Stimulate gluconeogenesis, glycogenolysis;
Anti-inflammatory, acts by dec Phospholipase A2, dec cytokines, dec histamine;
Periphery - [oppose insulin] dec glu use, inc proteolysis, lipolysis;
Mostly delayed effects;
90% bound to CBP or albumin;
Converted (kidney, colon, salivary glands) to cortisone - won't bind MC receptors; |
|
|
Term
| Betamethasone (Celestone) |
|
Definition
Glucocorticoid;
Long t1/2;
Oral, topical admin;
Tx asthma |
|
|
Term
| Aminoglutethimide (Cytadren) |
|
Definition
Adrenocortical "inhibitor";
Inhibits CYP450 - Dec cortisol production;
Tx Cushings |
|
|
Term
| Ethinyl estradiol (Estinyl) |
|
Definition
Estrogen - synthetic 17alpha;
Dec first pass met;
Tx CONTRACEPTION (most common Rx) |
|
|
Term
|
Definition
Synthetic progesterone;
Tx endometrial cancer, component of birth control |
|
|
Term
|
Definition
SERM;
Agonist in bone, brain, liver;
Antagonist in breast, endometrium;
Tx breast & endometrial cancers |
|
|
Term
|
Definition
SERM;
Agonist in bone, brain, liver;
Antagonist in breast, endometrium;
Tx breast & endometrial cancers |
|
|
Term
|
Definition
Anti-estrogen;
Antagonist in all tissues (ER-alpha & -beta);
Ovulation induction via reflex inc GnRH;
Tx infertility |
|
|
Term
|
Definition
Anti-estrogen;
Antagonist in all tissues (ER-alpha & -beta);
Ovulation induction via reflex inc GnRH;
Tx infertility |
|
|
Term
| Mifepristone (Mifeprex) - RU 486 |
|
Definition
Anti-progestin;
Blocks P receptor for the termination of gestation in first 7 weeks |
|
|
Term
|
Definition
Aromatase inhibitor;
Block production of estrogens from androgens;
Tx breast cancer after Tamoxifen fails |
|
|
Term
|
Definition
Androgen;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, PMS, anabolic steroids;
SE - masculinization, virilization, CAD, hepatic carcinoma, suppression of LH & FSH |
|
|
Term
| Methyltestosterone (Oretin methyl) |
|
Definition
Testosterone derivatve;
Oral, short acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx elderly men (inc muscle mass), IM injection for HRT, endometriosis, anabolic steroids; |
|
|
Term
|
Definition
Testosterone derivatve;
IM, long acting;
[A] Bind androgen receptor - transcriptional regulation;
[B] Conv to DHT - inc potency;
[C] Conv to estradiol - closes epiphyseal plates;
Tx ENDOMETRIOSIS, elderly men (inc muscle mass), IM injection for HRT, endometriosis, PMS, anabolic steroids; |
|
|
Term
| Cyproterone acetate (Cyprostat) |
|
Definition
Androgen receptor antagonist;
Competes with DHT;
Tx acne, baldness, virilizing syndrome, sexual deviants (dec libido) |
|
|
Term
|
Definition
Androgen receptor antagonist;
Tx prostate cancer;
SE - hepatotox |
|
|
Term
|
Definition
(also Propecia);
Blocks testo conversion (5alpha reductase) to DHT;
Tx BPH, male-pattern baldness;
SE - teratogenic |
|
|
Term
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
1st Gen. Sulfonylurea;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
2nd Gen Sulfonylurea - 10-100X more potent;
Oral admin, rapidly absorbed, extensive protein binding;
Acts @K+ channel;
Initially inc insulin release;
Inc insulin sensitivity, inc glu uptake;
Tx DM, promote hypoglycemia;
Interaxn w/ NSAIDs |
|
|
Term
|
Definition
Meglitinide - benzoic acid deriv;
Very rapid GI absorption;
Inc insulin secretion;
Short t1/2, used for post-prandial control
Tx DM, promote hypoglycemia;
SE - severe hypoglycemia; |
|
|
Term
|
Definition
Biguanide;
GI absorption - little first pass met.;
Dec hepatic glucose production;
No hypoglycemia, NO INSULIN AXN;
SE - BLACK BOX lactic acidosis |
|
|
Term
|
Definition
Thiazolidindione;
GI absorption - little first pass met.;
Bind PPAR-gamma receptor, inc insulin sensitivity;
Tx DM, promote hypoglycemia; |
|
|
Term
|
Definition
Alpha-glucosidase (brush border enzyme) inhibitor;
Dec carbohydrate (starch) absorption;
Dec post-prandial glu spike;
Tx DM, promote hypoglycemia; |
|
|
Term
|
Definition
Incretin- Works thru GIP/GLP-1 mechanisms, more potent;
Synthetic version of exendin-4 (Gila monster);
Inc insulin, dec glycogenolysis, dec gastric emptying, dec appetite, dec glucagon, some inc in beta cells - hypoglycemia!; |
|
|
Term
|
Definition
Calcitriol mimetic;
Conv in body to calcitriol;
Tx - rickets, osteomalacia, hypoparathyroid, osteoporosis |
|
|
Term
|
Definition
Calcitriol analog;
Tx PSORIASIS(better than GCs), rickets, osteomalacia, hypoparathyroid, osteoporosis |
|
|
Term
|
Definition
1st Gen. Bisphosphonate;
Less effective orally;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, hypercalcemia;
SE - via IV admin, osteonecrosis of jaw (less common in 1st gen) |
|
|
Term
|
Definition
2nd Gen. Bisphosphonate - more potent;
Most common Rx for post-meno Tx;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis;
SE - via IV admin, osteonecrosis of jaw (less common in 2nd gen), irritation of esophagus |
|
|
Term
|
Definition
3rd Gen. Bisphosphonate - HIGH POTENCY;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, BONE CANCER;
SE - via IV admin, osteonecrosis of jaw! |
|
|
Term
|
Definition
3rd Gen. Bisphosphonate - HIGH POTENCY;
Analog of inorganic pyrophosphate;
Take in morning, without food;
Inhibits bone resorption;
Tx - Pagets, osteoporosis, BONE CANCER;
SE - via IV admin, osteonecrosis of jaw! |
|
|
Term
|
Definition
Calcimimetic - Ca sensing receptor mimetic;
Binds allosterically to the receptor, suppresses PTH;
Tx hyperparathyroid w/ PT-carcinoma |
|
|
Term
|
Definition
Anti-Protozoal;
Activation via enzymatic reduction;
Blocks pyruvate:ferrodoxone oxidoreductase;
90% bioavail, BBB penetration, low protein binding;
Tx - trichomonas, entamoeba h., giardia, anaerobes (B. fragilis, C. diff);
SE - GI, HA, metallic taste, dizziness, disulfriam-like, anorexia, neuro tox |
|
|
Term
|
Definition
Anti-Protozoal;
Inhibits electron transport, dec pyrimidine synth;
99% protein bound, lipophillic, hydrophobic;
Tx pneumocystic pneumonia, toxoplasma, entamoeba, trichomonas, P. falciparum |
|
|
Term
|
Definition
Anti-Protozoal;
Oral (50% bioavail) or IV admin;
Inh ornithine decarboxylase to block polyamine synth;
Tx - W. trypanosoma
SE - anemia, leucopenia, diarrhea, convulsions, GI, alopecia |
|
|
Term
|
Definition
Blood schizontocide;
Wide distribution, slow clearance (months);
Resistance - efflux at P-gp;
Tx - Plasmodium, non-GI amebiasis;
Prophylactic use;
SE - blurred vision (melanin binding, corneal deposits), retina pigmentation, hemolysis (if G6PD deficient); |
|
|
Term
|
Definition
Blood schizontocide;
Block DNA synthesis;
Tx - P. falci, gametes of P. vivax and P. malariae;
Poor therapeutic index;
SE - dec heart contract., dilate vessels, contract uterus, vertigo, hemolysis (if G6PD deficient),
Cinchonism - tinnitus, blurred vision, HA, dec hearing |
|
|
Term
|
Definition
Blood schizontocide;
Oral admin, 98% bound, excreted in bile;
Acts only @ asexual erythrocytic stages;
Block DNA synthesis;
Tx - P. falci, gametes of P. vivax and P. malariae;
SE - GI, vertigo, convulsions;
CI - BBs, chloroquine, quinine, quinidine, hx seizures |
|
|
Term
|
Definition
Blood schizontocide - Attack plasmodia in red blood cells preventing or terminating the clinical attack;
Acts only @ asexual erythrocytic stages; |
|
|
Term
|
Definition
Tissue schizontocide, Gametocidal, Hypnozoitocidal;
Rapidly abs and conv to Carboxyprim.;
Tx - prophylaxis, P. vivax and P. ovale @ hepatic and gamete stages;
KILLS P. FALCI GAMETES;
CI - G6PD deficient (X-linked) leads to hemolytic anemia |
|
|
Term
|
Definition
Tissue schizontocide;
High abs;
Inhibits DHFR;
SE - dec hematopoeisis, megaloblastic anemia;
Never used alone, oft w/ Sulfadoxine |
|
|
Term
| Fansidar (Sulfadoxine/Pyrimethamine) |
|
Definition
Tissue schizontocide axn;
Tx - chloro-resistant P. falci, Toxoplasma;
SE - fatal cutaneous rxns (incl erythema multi, SJS, epidermal necrolysis); |
|
|
Term
|
Definition
Benzimidazole - Anti-helmintic;
Rapid met to albendazole sulfoxide;
Inh carb transport and microtubule assembly - immobilization and death;
Blocks larval development;
Tx helmintics - ascariasis, enterobius, hookworm;
SE - teratogen |
|
|
Term
|
Definition
Benzimidazole - Anti-helmintic;
Poor abs, highly bound;
Inh carb transport and microtubule assembly - immobilization and death;
Blocks larval development;
Tx helmintics - ascariasis, enterobius (pin), Trichuris (whip), hookworm;
SE - teratogen |
|
|
Term
|
Definition
Anti-helmintic;
Inc Ca++ perm - spastic paralysis;
Readily abs, hi first pass met, inc metabolites;
Tx - tapeworms, schistosomiasis, 3 forms of fluke;
SE - GI, HA;
CI - Carbamazepine & Phenobarbital dec bioavail; Cimetidine inc bioavail, ocular schistosomiasis; |
|
|
Term
|
Definition
Anti-helmintic;
Oral admin, no met, long t1/2 (slow cl);
Inc Cl perm. - inh glutamate and GABA-ergic channels - paralysis;
Tx - strongyloidiasis, onchocerca (rvr blindness);
SE - GI, itch, dizzy, inflamm rxn to dying bugs |
|
|
Term
|
Definition
Anti-helmintic;
Rapid GI abs;
Tx lymphatic filariasis;
SE - anorexia, nausea, HA |
|
|
Term
|
Definition
Anti-helmintic;
Poor abs;
Bind N receptors - depol blockade - spastic paralysis (bug falls off GI wall);
Tx - MONILIFORMIS, GI nematodes;
Dec SE due to localization of drug in GI - HA, dizziness, rash |
|
|
Term
| Cholestyramine (Questran) |
|
Definition
Bile acid sequesterants;
Powder form;
Anionic, binds (-) bile acids in GI - inh bile recycling - liver excretes more chol;
Safe for children, hepatic dz;
Dec LDL by 25%;
SE - sandy texture, flatulence, hypertriglyceridemia, constipation, drug interaction; |
|
|
Term
|
Definition
Statin - inh HMG-CoA Reductase;
Prodrug, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases, INTERAXN @ CYP3A4;
CI - renal dz |
|
|
Term
|
Definition
Statin - inh HMG-CoA Reductase;
Inc potency, dec renal cl, intestinal reabsorb by P-gp;
Inh chol. synthesis in liver - inc # of LDL receptors - clearance of VLDL and LDL from blood;
Dec LDL by 60%;
SE - GI, sleep disrup, teratogenic, rhabdomyolysis, myositis, myalgia, inc aminotransferases, INTERAXN @ CYP3A4; |
|
|
Term
|
Definition
Cholesterol absorption inhibitor;
Blocks internalization of NPC1L1 - dec chol abs by 50% - dec hepatic chol - upreg of LDL receptors - dec LDL by 18%;
SE - GI, fatuge, gallstones, Category C, inc liver enzymes;
Inc lvls in elderly, female;
CI - <10y.o., hepatic or renal insuff, lactation |
|
|
Term
|
Definition
Fibrate - anti-lipid;
Active met - fenofibric acid - glucaronidation;
Activate PPAR-alpha - FA oxidation, inc biliary chol excretion (Dec TG by 50%);
Inc HDL (Apo-A1), no effect on LDL!;
SE - gallstones, inc transaminases, dec GFR, azotemia;
CI - renal dz |
|
|
Term
|
Definition
Anti-lipid;
Dec FFA mobilization - dec TG & ApoB synth (dec VLDL), inc HDL transport, enhanced LPL;
Dec LDL by 25%, Dec TG by 50%, Dec Lp(a);
Dec CHD/MI incidence;
SE - hepatotox (inc enzymes), flushing, conjunctivitis, retinal detach, inc insulin resistance (a. nigricans), gout, dry skin, Category C, pruritis |
|
|
Term
| Levothyroxine (Synthroid) |
|
Definition
L-T4;
Most common Rx;
Calorigenic, inc HR, cardiac contraction force |
|
|
Term
|
Definition
L-T4 and L-T3;
Calorigenic, inc HR, cardiac contraction force |
|
|
Term
|
Definition
Thioureylenes - anti-thyroid;
[1] Inh I organification (via peroxidases), can't bind to thyroglobulin;
[2] Inh periph. (liver) conversion of T4->T3;
Tx hyperthyroidism;
SE - agranulocytosis, rash;
Less likely to cross placenta, use caution |
|
|
Term
|
Definition
Thioureylenes - anti-thyroid;
Inh I organification(via peroxidases), can't bind to thyroglobulin;
10X more potent and longer t1/2 than PTU;
Tx - hyperthyroidism
SE - teratogen |
|
|
Term
| Radioactive iodine, Na-131I |
|
Definition
Oral admin;
In thyroid, beta-radiation will destroy parenchymal cells, minimum collateral dmg;
Adult usage, but not in women of child-bearing age;
Tx enlarged thyroid (Graves, goiter) |
|
|
Term
|
Definition
Inh periph (liver, kidney, pituitary, brain) conv of T4->T3;
Tx hyperthyroidism (off-label) |
|
|
Term
Marijuana
(Cannabis sativa) |
|
Definition
Delta-9-THC psychoactive compound;
cannabinol (CBN) less active metabolite, cannabidiol (CBD) anxiolytic;
Retrograde transmission - inc extracellular K, block Ca++ influx, ↓NT release, dec cAMP leads to tolerance;
SE - psychotoxicity, carcinogenic (SCC), teratogenic |
|
|
Term
|
Definition
Acute - ↓memory, confusion, depersonalization, ↑ hunger, ↓REM, ↓ balance, dry mouth
EARLY High:Euphoria, laughter time distortion
LATE: relaxation, introspection, dream like state
Chronic - amotivational syndrome, apathy, dullness, ↓concentration, ↓memory
Tolerance:↓adenylate cyclase (cAMP), ↓receptors (CB1, CB2) cross tolerance with opiods and EtOH |
|
|
Term
| Cardiovascular effects of Marijuana |
|
Definition
|
|
Term
| Immune effects of Marijuana |
|
Definition
↓ T-cells; suppress immune response
Via CB2 receptor on lymphocytes and macrophages |
|
|
Term
| Endocrine effects of Marijuana |
|
Definition
↓ LH and FSH - ↓ testosterone, testes♂, ↓ libido;
↓GH, ↓ Prl, ↑ACTH;
Anovulatory cycles♀ |
|
|
Term
| Respiratory effects of Marijuana |
|
Definition
Acute - bronchodilates;
Chronic - bronchoconstricts |
|
|
Term
| Withdrawl effects of Marijuana |
|
Definition
Irritable,
Nausea,
Insomnia,
Sweating,
Anorexia,
Hand tremor,
Restlessness |
|
|
Term
|
Definition
Medical marijuana; NATURAL product extracted THC
Approved Use: Antiemetic during chemo, AIDS wasting syndrome;
Possible - MS, spinal injury, Tourette's, dyskinesias |
|
|
Term
LSD
(lysergic acid Diethylamide |
|
Definition
5-HT2 partial agonist;
Physio - sympathomimetic;
Psychic - visual hallucinations, time/sense alter, loss of boundaries, emergence of thoughts/memories, 'magically in control', synesthesia
SE-Bad trip, persistent rx with BNZ, sober flashbacks |
|
|
Term
Mescaline
3,4,5-trimethoxyphenethylamine |
|
Definition
Psychedelic alkaloid, 5HT and DA agonist;
Physio - Sympathomimetic;
Psychic - hallucinations, unusual time perception;
SE - paranoia and fear
Schedule 1 drug |
|
|
Term
|
Definition
Cactus known for containing Mescaline
Peyote Buttons |
|
|
Term
|
Definition
PCP, Angel Dust;
NMDA receptor antagonist, Sigma receptor agonist, Dopamine/NE reuptake inhibitor;
Physio - sympathomimetic;
Psychic - Inc sensitivity to stimuli, dec proprioception, restlessness, mood elevation, disorientation, detachment, anxiety, perceptual disturbance, detachment;
Tox - hostility, confusion, coma, schizo, behavorial |
|
|
Term
|
Definition
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
CI - oral lesions, active smoking |
|
|
Term
| Nicotine Patch (Habitrol) |
|
Definition
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 |
|
|
Term
|
Definition
Nicotine receptor partial agonist, non-nicotine cessation aid;
High affinity @ alpha4-beta2-cont. receptors; some affinity @ 5HT-3;
25% @ 12 mos rmain quit, 2nd line tx after Buproprion
SE: BB warning suicidal ideation, nausea |
|
|
Term
|
Definition
Non-nicotine cessation aid; Anti-HTN medication
Non-selective antagonist a non-alpha7-N cholinergic receptors;
Crosses BBB;
Action @ brain and peripheral ganglia - ↑ SE's;
Inconclusive efficacy, use w/ patch; |
|
|
Term
|
Definition
NMDA antagonist, alters ion channels – initial excitatory then depressive;
diff channels effected at diff concentrations of intox;
Detox req ADH and ALDH enzymes;
Women - dec gastric first pass met and ↓ ADH levels;
SE - CNS dmg, hepatomegaly, vasodilation, cardiomyopathy, pancreatitis, anemia, bone marrow suppression, teratogenic;
CI – NSAIDs |
|
|
Term
| Ethanol CNS damage, mechanisms |
|
Definition
Thiamine B1 deficiency - beriberi;
Wernicke's encephalopathy - nystagmus, ocular palsies, ataxia, gait;
Korsakoff's psychosis - confabulation; antero and retrograde amnesia
Cerebellar degen - 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 |
|
|
Term
|
Definition
Early: agitation, confusion, hyperactive ANS, seizure(2-48hrs)
Late: Delirium Tremons- hyperthermia, hallucination, disorientation;
Coma, death
Trx: BNZ, phenytoin, Phenobarbital (siezures) atenolol, clonidine |
|
|
Term
|
Definition
Wood alcohol;
Oxidized to form FORMALDEHYDE(!) and formic ACID
SE - blindness, irreversible acidosis, death;
Tx OD w/ ethanol (competitive substrate) and dialysis, treat acidosis |
|
|
Term
|
Definition
Vitamin B1
Should admin to all alcoholics in distress;
Replacement for thiamine lost in deficient state
Deficiency is Beriberi Wet=CV complications Dry=CNS complications, B1 involved in glucose metabolism , lethargy, neuropathy, GI complications and arrythmias |
|
|
Term
|
Definition
ALDH antagonist - ↑acetaldehyde;
Inhibits DA beta-hydroxylase (↓ NE);
Acetaldehyde syndrome - ↑HR, flush, hypotension, N/V, HA;
NO effect on cravings
Tx - chronic alcoholism;
SE - hepatotoxcity, depression, psychosis |
|
|
Term
|
Definition
Opioid receptor antagonist;
LONG DURATION (24 hrs) effect t1/2=4 hrs
oral admin, extensive first pass;
tx alcohol abuse (↓craving and ↓ relapse);
↓ number of 'heavy drinking days' |
|
|
Term
|
Definition
Anti-emetic - 5-HT3 antagonist;
Dec craving by blocking the reward pathway;
Tx - chronic alcoholism; |
|
|
Term
|
Definition
AMPA-R antagonist, GABA-R regulator;
Tx - chronic alcoholism;
Dec 'heavy drinking days';
Need to titrate dosing;
SE – glaucoma |
|
|
Term
|
Definition
Tx EtOH withdrawal stages...
tremulousness syndrome,
DT |
|
|
Term
|
Definition
Oral or IV;
Tx Acetaminophen OD when >[150mg/mL] @ 4hrs OR >[75mg/mL] @ 8 hrs;
Use in first 10 hrs;
SE - anaphylaxis, N/V, taste/odor; |
|
|
Term
|
Definition
Benzodiazepine antagonist;
Tx BNZ OD;
Can produce withdrawal symptoms, not used too often;
SE - N/V, dizzy, panic attacks, seizures, blurred vision |
|
|
Term
| Physostigmine (Antilirium) |
|
Definition
reversible anticholinesterase;
tx atropine O.D., other anticholinergic (antidepressant, antihistamine, antiemetic, antipsychotics) OD
crosses BBB, CNS stim then depression;
CI - TCA's |
|
|
Term
|
Definition
Tx organophoshate (insecticide) OD;
Use with supportive tx |
|
|
Term
|
Definition
reactivator of cholinesterase;
Slow IV admin;
Tx organophosphate, sarin, soman OD!;
Rapid admin SE's - NM block, msucle spasm, HTN, tachycardia |
|
|
Term
|
Definition
Chelator used in OD Tx of lead (mild cases, approved for children), arsenic, and mercury (inc mercury excretion in vapor exposure);
Reduces blood lvls, can't repair damage;
SE - hypersensitivity |
|
|
Term
|
Definition
Chelator;
First line tx for arsenic poisoning;
Also Tx lead, mercury poisoning;
SE - nephrotoxic;
CI - G6PD deficiency |
|
|
Term
|
Definition
Iron chelator;
Tx - first line for iron tox;
SE - red urine, tachycardia, hypoT, abdominal pain, N/V, flush, fever |
|
|
Term
|
Definition
TCA (tertiary amine);
Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation;
VERY SEDATING, ANTICHOLINERGIC;
Blocks mAch, 5-HT, and histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility;
Low therapeutic index;
SE - orthostatic hypoT, tachycardia, confusion, anticholinergics, worsen narrow-angle glaucoma and CHF, acidosis, delirium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) |
|
|
Term
|
Definition
TCA (tertiary amine);
Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation;
Blocks mAch, 5-HT, and histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility;
low therapeutic index;
CYP2D6, conjugation
SE - orthostatic hypoT, tachycardia, confusion, anticholinergics, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine |
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Term
|
Definition
TCA (secondary amine);
Inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation;
LITTLE sedation;
Blocks mAch, NO 5-HT EFFECT, and little histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility;
Low therapeutic index;
SE - orthostatic hypoT, tachycardia, confusion, anticholinergics, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) |
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Term
|
Definition
Atypical antidepressant;
2nd Generation NO sedation NO anticholinergic;
MOA uncertain, blocks NE reuptake, weak blocker of DAT, SERT, NET;
SE - anxiety, restlessness, seizure;
Can be used in smoking cessation |
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Term
|
Definition
Atypical antidepressant - 3rd generation;
STRONG SEDATION;
Antagonizes presynaptic α-2 receptors [unique] - ↑ release of serotonin and NE; NOT MDR-1 substrate;
Antagonizes 5-HT2 receptors, Anti-histamine action;
SE - sedation, weight gain; |
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Term
|
Definition
Atypical antidepressant - 3rd Generation;
POTENT anticholinergic
5-HT reuptake inhibitor, NO NE effect;
INHIIBITS CYP3A4;
Tx depression w/ sleep disturbance and/or anxiety; |
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Term
|
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
Tx - MDD, panic attack, OCD, ADHD ….
Long t1/2 - 3 days;
High therapeutic index;
SE - nausea, dec libido;
LEAST side effects of SSRIs;
CI - MAOI, amphetamines, ecstasy, LSD, L-tryptophan;
Serotonin syndrome! |
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Term
|
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
Long t1/2 - a WEEK!;
High therapeutic index;
NOT MDR-1 substrate;
SE - nausea, dec libido;
CI - MAOI, amphetamines, ecstasy, LSD, L-tryptophan;
Serotonin syndrome!
MAY ↑levels of lithium, warfarin and TCA |
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Term
| Tranylcypromine (Parnate) |
|
Definition
MAOI - 2nd line anti-depressants;
also Tx - panic disorder, agoraphobia;
Irreversibly inhibits oxidative metabolism of monoamines (NE, 5-HT) ↑ stores in vesicles and released;
Acute: CNS Stimulation, agitation euphoria possible
Requires daily dosing due to inactivation;
SE - orthostatic hypoT sleep disturbance, agitation;
CI - cheeses (tyramine) EtOH, Beer, sympathomimetics [Acute HTN], Meperidine, dextromethorpham, SSRIs |
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Term
|
Definition
MAOI - 2nd line anti-depressants;
also Tx - panic disorder, agoraphobia;
Irreversibly inhibits oxidative metabolism of monoamines (NE, 5-HT) ↑ stores in vesicles and released;
Acute: CNS Stimulation, agitation euphoria possible
Requires daily dosing due to inactivation;
SE - orthostatic hypoT sleep disturbance, agitation;
CI - cheeses (tyramine) EtOH, Beer, sympathomimetics [Acute HTN], Meperidine, dextromethorpham, SSRIs |
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Term
|
Definition
MAOI - 2nd line anti-depressants;
also Tx - panic disorder, agoraphobia;
Irreversibly inhibits oxidative metabolism of monoamines (NE, 5-HT) ↑ stores in vesicles and released;
Acute: CNS Stimulation, agitation euphoria possible
Requires daily dosing due to inactivation;
SE - orthostatic hypoT sleep disturbance, agitation;
CI - cheeses (tyramine) EtOH, Beer, sympathomimetics [Acute HTN], Meperidine, dextromethorpham, SSRIs |
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Term
|
Definition
Mood-stabilizer;
First line in treating Bipolar;
Unknown MOA - may block inositol P signal and AC activity;
Rapid absorption, NOT metabolized, renal clearance - t1/2 = 20 hrs;
NARROW THERAPEUTIC WINDOW;
SE - tremor, ataxia, hyperactive, aphasia, sedation, edema, hypothyroid, nephrogenic DI, cardiac sick sinus syndrome [bradycardia], acne, folliculitis, ↑psoriasis;
CI: NSAIDS alter renal elimination |
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Term
|
Definition
BRA - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA;
Specific for BZ-1 receptor at approved doses;
Pregnancy category C (Okay, but caution), schedule IV; |
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Term
|
Definition
BRA - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA;
Specific for BZ-1 receptor at approved doses;
Pregnancy category C (Okay, but caution), schedule IV;
ETHNIC VARIABILITY - Asians, must ↓ the dose ALDH |
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Term
|
Definition
HIV Fusion Inhibitor - by binding gp41 of viral envelope;
Admin SQ, 2X a day;
Met by proteolytic hydrolysis, no CYP rxns;
No cross resistance with OTHER drugs;
Only for tx-experienced pts;
SE - inc risk of bacterial pneumonia |
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Term
|
Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (pyrimidine-T) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Dec perinatal HIV transmission;
Met by glucaronidation;
Avoid fatty meals (dec AUC);
SE - MYELOSUPPRESSION, lactic acidosis, lipodystrophy |
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Term
|
Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral;
Nucleoside analog (purine-A,G) forms active ddATP - act as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Don't take w/ acidic foods (dec AUC);
SE - PERIPHERAL NEUROPATHY, PANCREATITIS, lactic acidosis, lipodystrophy, many drug interaxns |
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Term
|
Definition
Nucleoside Reverse Transcriptase Inh (NRTI) - Anti-retroviral, Anti-HBV;
Nucleoside analog (pyrimidine-C) acts as competitive inhibitor - block elongation in previously uninfected cells;
Req (+P)X3 for axn;
Longest NRTI t1/2;
SE - lactic acidosis, lipodystrophy |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION - but least in class;
LARGE AUC if taken w/ meals;
SE - hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Protease inhibitor - Anti-retroviral;
Most eff. ART - competitive, reversible, inh of protease binding site, esp in monocytes, macrophages - blocks MATURATION;
CYP3A4 INHIBITION - most potent;
SE - HEPATOTOX, hyperlipid, DM, lipodystrophy, inc liver enzymes, inc bleeding in hemophliacs; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Purine analog;
Tx - HSV, VZV, CMV;
Req (+P) by VIRAL thymidine kinase;
SE - HA, nausea, diarrhea, renal, CNS: tremors, delirium, seizures; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Acyclovir prodrug - Purine analog;
Tx - HSV, VZV, CMV;
Req (+P) by VIRAL thymidine kinase;
SE - HA, nausea, diarrhea, renal, CNS: tremors, delirium, seizures; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - COMPETITIVE INH, NO chain termination;
Penciclovir prodrug - guanine analog;
Tx - HSV, VZV, CMV, also HBV;
Req (+P) by VIRAL thymidine kinase; |
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Term
|
Definition
Anti-Herpes - Nucleoside analog;
Inh viral DNA pol - chain termination;
Tx - CMV DOC, CMV RETINITIS;
Req (+P) by VIRAL thymidine kinase;
100X more potent than Acyclovir;
SE - MYELOSUPP., TERATOGENIC, HA, nausea, diarrhea; |
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Term
|
Definition
Anti-Herpes - NucleoTIDE analog;
No (+P) by viral TK;
Tx - HSV, VZV, CMV RETINITIS;
SE - NEPHROTOX, neutropenia, carcinogenic, ocular hypotony |
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Term
|
Definition
Pyrophosphate analog - Anti-Herpes;
"Non-nucleoside";
Inh DNA pol by blocking cleavage, ALSO Inh HIV-RT;
NO (+P) required;
Tx - nucleoside resistant cases (HSV, VZV, CMV), CMV retinitis;
SE - NEPHROTOX, N/V, anemia, fatigue |
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Term
|
Definition
Anti-hep - nucleoside analog (G);
Competitive inh of GTP 5' capping of viral mRNA;
Concentrates in RBCs;
Tx - HCV, RSV;
SE - hemolytic anemia, teratogenic, myelosupp. |
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Term
|
Definition
Anti-Parkinsonism, Anti-flu - Uncoating inh;
Blocks HA glycoprotein maturation - blocks binding to M2 ion channel;
No internal acidification;
Work on Flu-A ONLY;
Enhances DA release;
"Good alternative to flu vaccine";
SE - restless, depression, psychosis, hallucinations, confusion;
CI - seizures, heart failure |
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Term
|
Definition
Anti-flu - Viral Release Inh;
Inh viral neuraminidase - no cleavage of sialic acid - destroys receptors recognized by HA - no detachment from host cell;
Admin via inhalation (low PO bioavail);
Tx flu-A(2nd line) and B |
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Term
| Chloropromazine (Thorazine) |
|
Definition
Typical Anti-Psychotic - low potency;
Inh of D2 receptor - effective for positive symptoms;
Aliphatic side chain - low potency (dec risk of EPS, inc risk of anti-muscarinic effects);
Tx for Huntington's chorea(DA antagonism;
SE - corneal deposits, INC PRL (severe), DEC INSULIN, JAUNDICE, ANTI-DIURETIC, ORTHOSTATIC hypoT, skin rxns, EPS |
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Term
|
Definition
Typical Anti-Psychotic;
Inh of D2 receptor - effective for positive symptoms;
Piperdine ring;
Dec incidence of EPS;
SE - inc PRL, highly anti-muscarinic |
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Term
|
Definition
Typical Anti-Psychotic - hi potency;
Inh of D2 receptor - effective for positive symptoms;
Tx for Huntington's chorea(DA antagonism);
SE - EPS, inc PRL |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Limited EPS;
SE - BLOOD DYSCRASIAS (esp leukopenia), inc risk of DM typeII, WEIGHT GAIN; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Tx CHILDREN AND TEENS;
Limited EPS;
SE - inc PRL, inc risk of DM typeII, METABOLIC SYNDROME; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
SE - WEIGHT GAIN, METABOLIC SYNDROME (hi incidence), inc risk of DM typeII; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2 (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
No effect on PRL levels;
SE - METABOLIC SYNDROME, inc risk of DM typeII; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 and 5-HT2A,1A,2C (high affinity) antagonism;
Inc efficacy for Negative symptoms (as well as positives);
Limited EPS;
SE - inc risk of DM typeII; |
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Term
|
Definition
Atypical Anti-Psychotic;
D2 partial agonist, 5-HT2 antagonist, and 5-HT1A partial agonist;
Inc efficacy for Negative symptoms (as well as positives);
No effect on PRL levels;
SE - inc risk of DM typeII; |
|
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Term
| CNS effects of Anti-Psychotics (6 sites) |
|
Definition
Cortex - dec seizure threshold;
Basal ganglia - inc DA metabolism, inc Ach turnover;
Limbic - main site of anti-psychotic efx;
Hypothalamus - inc PRL;
Brainstem - dec reflexes;
CTZ - protect AGAINST N/V |
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|
Term
| Endocrine effects of Anti-Psychotics |
|
Definition
|
|
Term
| Cardiovascular effects of Anti-Psychotics |
|
Definition
Direct and indirect effects;
Orthostatic hypotension - esp chlorpromazine |
|
|
Term
| EPS of of Anti-Psychotics (6) |
|
Definition
Acute dystonia;
Akathesia;
Parkinsonian syndrome;
Neuroleptic Malignant Syndrome;
Perioral tremor;
Tardive dyskinesia |
|
|
Term
| Anti-cholinergic effects of Anti-Psychotics |
|
Definition
Dry mouth;
blurred vision;
constipation;
nasal congestion;
orthostatic hypoT |
|
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Term
|
Definition
Parkinsonism Tx;
Allowed to cross BBB and Conv to DA by endogenous L-AAD @CNS AND peripherally (large dose req'd);
First line for Park. but can only use 3-5 years;
SE - anorexia, orthostatic hypoT, arrhythmias (Afib), tachycardia;
CI - Vit B6, MAOI, glaucoma, psychosis, ulcers CV dz |
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|
Term
| L-DOPA/carbidopa (Sinemet) |
|
Definition
Parkinsonism Tx;
L-DOPA fxn PLUS...
Peripheral inh of L-AAD - dec amt of L-DOPA req for therapy;
Fluctuating responses;
SE - depression, anxiety, delusions, chorea, tics;
CI - Vit B6, MAOI, glaucoma, psychosis, ulcers CV dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D2 agonist, D1 partial agonist;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D1/D2 agonist, inc efficacy;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - DA receptor agonist;
Activate D2 - dec activation of indirect basal ganglia pathways;
D2 selective agonist;
Tx EARLY dz |
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Term
|
Definition
Parkinsonism Tx - COMT inhibitor;
Prolong axn of L-DOPA and dec it's transport-competitor 3OMD;
PERIPHERAL AXN;
Preferred due to dec SE's |
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Term
|
Definition
Parkinsonism Tx - Anti-muscarinic;
Alter DA/Ach balance by blocking Ach-stimulation of striatum;
Tx early Park or as adjunct to L-DOPA;
SE - drowsy, inattention, delusions, hallucinations, typical ANS anti-Ach axns |
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Term
| Diphenhydramine (Benadryl) |
|
Definition
Parkinsonism Tx - Anti-muscarinic;
Alter DA/Ach balance by blocking Ach-stimulation of striatum;
Tx early Park or as adjunct to L-DOPA;
SE - drowsy, inattention, delusions, hallucinations, typical ANS anti-Ach axns |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
Long t1/2 - 70hrs;
SE - GI, insomnia, bradycardia |
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Term
|
Definition
Alzheimer's Dz Tx - Ach-esterase Inh;
Inc lvls of Ach;
SE - GI, insomnia, bradycardia |
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Term
|
Definition
ALS tx;
Dec Glu release by (1) block inactive Na-channel, (2) block activated Ca-channel;
Also (3) block NMDA channel;
Met by CYP1A2;
Hi protein binding;
SE - fatigue, sedation, liver dz |
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Term
|
Definition
MS tx - Anti-inflamm;
Restores BBB - dec immune response in CNS;
More effective than interferon;
Tx also Crohn's;
SE - PML!! (progressive multifocal leukoencephalopathy) |
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Term
|
Definition
Anti-Epilepsy - Hydantoin;
Stabilizes inactive Na channels;
Met by CYP2C4, induces 2C and 3A;
Highly protein bound - competes w/ other drugs (warfarin, OCT, carbamazepine);
SE - [narrow TI] nystagmus, ataxia, arrhythmias, coarsened face, hirsutism, gingival hyperplasia, peripheral neuropathy, bone disruption, teratogenic |
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Term
|
Definition
Anti-epilepsy - barbiturate;
Prolong opening of GABA receptor;
Blocks AMPA receptor;
Induce CYP2b6 and UGT;
SE - sedation, lethargy, nystagmus, rash, megaloblastic anemia, dec vitD |
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Term
|
Definition
Anti-epilepsy - iminostilbenes;
Mood-stabilizer;
Prolongs Na channel recovery;
Met by CYP2C9,3A4 to active 10,11-epoxide;
Induces CYP1A2, 2B6, 2C19, UGT;
Tx - DOC for partial seizures, T/C, mood stabilizer for bipolar, trigeminal neuralgia;
Tx depression typically assoc w/ Huntington's;
SE - blood dyscrasias, diplopia, ataxia |
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Term
|
Definition
Anti-epilepsy - succinimides;
Inh of T-type Ca channels - prevents 3Hz spike/waves;
Inc AUC when given w/ valproic acid;
Met by hydroxylation;
Tx - DOC for absence seizures;
SE - [tolerance] euphoria, hiccups, fatigue |
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Term
|
Definition
Anti-epileptics - Carboxyllic acid;
Stabalizes inactive Na channels, Dec Ca current, stimulates GABA synth and inhibits degradation;
Met by UGT via beta-ox - also inhibits it;
Inh CYP2C9;
Tx - absence + T/C DOC, myoclonic, partial;
Inc [plasma] phenobarb, phenytoin, carbamazepine;
SE - heartburn, liver tox, teratogenic; |
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Can be given rectally;
Tx - refractory myoclonic, atonic, absence;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Tx - DOC status epilepticus;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epilepsy - BNZ;
Inc opening of GABA Cl channel;
Long acting, can admin rectally;
Tx - status epilepticus;
SE - sedation, lethargy |
|
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Term
|
Definition
Anti-epileptic;
Inh Na channels, inh T-type Ca channels;
Tx - parital seizures, infantile spasm, myoclonic, generalized and absence;
Met by CYP3A4; |
|
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Term
|
Definition
Muscle Relaxant;
GABA(B) agonist - inhibitory and hyperpolarization;
Inh substance P;
Admin oral or intrathecal;
Don't d/c abruptly - rebound neural hyperactivity;
Tx - spasticity, MS;
SE - sedation, CNS depression, hypoT |
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Term
|
Definition
Muscle Relaxant;
Pre-synaptic alpha2 agonist - dec axn of spinal motor neurons;
Admin oral - hi first pass met.;
Tx - spasticity, MS;
SE - SEDATION, hepatotox, anticholinergics, hypoT;
CI with other drugs acting on alpha2; |
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Term
|
Definition
Muscle Relaxant;
Blocks ryanodine receptor - confine Ca in sarcoplasmic reticulum - dec SKELETAL muscle axn;
Admin oral or IV - hepatic met (perform liver fxn tests);
Tx - spasticity, malignant hyperthermia, neuroleptic malignant syndrome;
SE - phlebitis, heptotox w/ estrogen, CNS depression, floppy child syndrome |
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|
Term
|
Definition
Muscle Relaxant;
CNS axn to sedate and dec pain, no direct efx on conduction;
Met by CYP2C19;
Tx - spasm;
SE - sedation, insomnia, vertigo, ataxia, vision loss, mydriasis, orthostatic hypoT |
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Term
|
Definition
Muscle Relaxant-ish;
GABA analog that binds to alpha-2-delta to inh neuronal Ca channels;
Dec neuropathic pain;
Tx - FIBROMYALGIA (muscle/joint pain);
SE - sedation, blurred vision, weight gain, swelling, xerostomia |
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Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - "Natural Pen";
Block cell wall-synth enzymes;
Oral admin;
Glomerular filtration, secretion;
Tx - G+ (staph, strep), GC, spirochetes (T. pallidum);
Res - B-lactamase (staph);
SE - rash, neurotoxic |
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Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam;
Block cell wall-synth enzymes;
Parenteral admin;
Glomerular filtration, secretion;
SE - rash, neurotoxic |
|
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Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - "Anti-staph";
Block cell wall-synth enzymes;
Parenteral admin;
Glomerular filtration, secretion;
Highly protein bound, acid stable;
Tx B-lactamase-producing staph;
SE - DEC ELECTROLYTES, rash, neurotoxic |
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Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - "Extended spectrum";
Block cell wall-synth enzymes;
Parenteral or oral admin;
Glomerular filtration, secretion;
Req supplement after dialysis;
Tx - [G+ and G- rods/bacilli] H. flu, E. coli;
Res - B-lactamase (G-);
SE - DELAYED RASH, DIARRHEA, PSEUDOMEMBRANOUS COLITIS, neurotoxic |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - "Extended spectrum";
Block cell wall-synth enzymes;
Oral admin;
Glomerular filtration, secretion;
Req supplement after dialysis;
Tx - [G+ and G- rods/bacilli] H. flu, E. coli;
Res - B-lactamase (G-);
SE - DELAYED RASH, PSEUDOMEMBRANOUS COLITIS, neurotoxic |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - 1st Gen Cephalosporin;
Renal tubular secretion - inc [plasma] w/ probenecid;
Tx - G+ cocci, many G- bacilli (think ampicillin);
SE - hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections; |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - 2nd Gen Cephalosporin;
Renal tubular secretion - inc [plasma] w/ probenecid;
Tx - H. flu, B. fragilis;
SE - hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections; |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - 3rd Gen Cephalosporin;
Renal tubular secretion - inc [plasma] w/ probenecid;
HIGHLY MET'D;
CROSSES BBB TO CSF;
Tx - [severe] enteric G-'s, B. fragilis, H. flu, Pseudo.;
SE - ENTEROBACTER SUPERINFECTIONS, hypersensitivity, phlebitis, IM pain, nephrotoxic; |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - 3rd Gen Cephalosporin;
Renal tubular secretion - inc [plasma] w/ probenecid;
LONGEST T1/2, HIGHLY PROTEIN BOUND - Dialysis OK;
CROSSES BBB TO CSF;
Tx - [severe] enteric G-'s, B. fragilis, H. flu, Pseudo.;
SE - ENTEROBACTER SUPERINFECTIONS, hypersensitivity, phlebitis, IM pain, nephrotoxic; |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth - B-lactam - 4th Gen Cephalosporin;
Renal tubular secretion - inc [plasma] w/ probenecid;
BROAD SPECTRUM - incl G+ w/ B-lactamase;
Tx - Pseudo, Klebsiella, E.coli;
SE - hypersensitivity, phlebitis, IM pain, nephrotoxic, rare superinfections; |
|
|
Term
|
Definition
Anti-Microbial - cell wall synth;
Cidal effects w/ narrow spectrum;
Oral admin for mild GI infxns, parenteral for systemic;
Enters inflamm meninges/CSF;
Res - plasmid-mediated alteration in binding site;
Tx - DOC for MRSA, strep, enterococci, 2nd line for C. diff;
SE - synergistic nephtrotox, ototoxicity (w/ loops), Red Man Syndrome, dec [plasma] in multiple myeloma, GI, phlebitis |
|
|
Term
|
Definition
Anti-Microbial - Inh 50S ribosome;
Oral admin (100% bioavail), also parenteral;
Supplement after dialysis;
Res - pt mutations of 23s RNA ribosome binding site;
Tx - VRE (E. faecium and faecalis)[static], MRSA [static], strep [cidal];
SE - N/V, diarrhea, pseudomembranous colitis, inh MAO;
CI - PKU |
|
|
Term
|
Definition
Anti-Microbial - 30S ribosome - "Tetracycline";
Passive diffusion thru porin channels into cell - ribosome binding;
Abs (best in stomach) inh by multivalent cations - enters placenta, milk;
Res - slow, via dec influx & inc efflux;
Tx [BROAD] - MYCOPLASMA, CHLAMYDIA, RICKETTSIAE, SPIROCHETES, protozoa, lyme, acne, peridontal dz;
SE - LIVER TOX, PHOTOSENS, TEETH discoloration, (LESS) GI, avitaminosis, vertigo, dec bone growth; |
|
|
Term
|
Definition
Anti-Microbial - 50S ribosome - "Macrolide";
Oral admin, STATIC axn;
Res [cross-res w/ Clinda] - rapid - plasmid-mediated dec influx, target altered, and drug hydrolysis;
Tx - [NARROW, G+] LEGIONAIRE'S DOC, Pneumociocci, GAS, Listeria, Corynebacterium, Lyme;
SE - CYP450 inh, cholestatic hepatitis |
|
|
Term
|
Definition
Anti-Microbial - 50S ribosome - "Macrolide";
Oral admin, STATIC axn;
DEC GI EFX, INC ACID STABILITY, INC ABS;
Res [cross-res w/ Clinda] - rapid - plasmid-mediated dec influx, target altered, and drug hydrolysis;
Tx - [NARROW, G+] Erythro's plus MAC'S DOC, H.flu, strep, H.pylori, Ct, Moraxella;
SE - CYP450 inh, cholestatic hepatitis |
|
|
Term
|
Definition
Anti-Microbial - 50S ribosome - "Macrolide";
Oral admin, STATIC axn;
LONG T1/2;
Res [cross-res w/ Clinda] - rapid - plasmid-mediated dec influx, target altered, and drug hydrolysis;
Tx - [NARROW, G+] DOC for LEGIONAIRE'S/MAC/CAMPYLOBACTER, H.flu, strep, Ct, Lyme;
SE - CYP450 inh, cholestatic hepatitis |
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Term
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Definition
Anti-Microbial - 50S ribosome - Sim. mech as macrolides;
Penetrates bone, not CSF;
Acid stable, slow resistance;
Tx - anerobes (B. FRAGILIS), G+, toxo, P. jiroveci;
SE - PSEUDOMEMBRANOUS COLITIS, GI, rash |
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Term
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Definition
Anti-Microbial - 30s ribosome (irrev. dmg) - aminoglycoside;
Diffuse through outer porin channel, req energy from ETC for cytoplasmic memb;
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 |
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Term
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Definition
Anti-Microbial - 30s ribosome (irrev. dmg) - aminoglycoside;
Diffuse through outer porin channel, req energy from ETC for cytoplasmic memb;
Conc-dependent killing - use bolus dose (parenteral);
Enters inflamm meninges/CSF, renal cortex, inner ear;
Limited cross-res within class;
Tx - [severe aerobic G-] P. aeruginosa;
SE - ototoxicity (irrev.), nephrotox (PCT, renal cortex), neuromuscluar blockade, teratogen |
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Term
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Definition
Anti-Microbial - 30s ribosome (irrev. dmg) - aminoglycoside;
Diffuse through outer porin channel, req energy from ETC for cytoplasmic memb;
Conc-dependent killing - use bolus dose (parenteral);
Enters inflamm meninges/CSF, renal cortex, inner ear;
Limited cross-res within class;
Tx - [resistant, severe aerobic G-] Klebsiella, Enterobacter, E.coli, 2nd-line TB!;
SE - ototoxicity (irrev.), nephrotox (PCT, renal cortex), neuromuscluar blockade, teratogen |
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Term
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Definition
Anti-Microbial - folic acid met;
Selective for bacterial enz DHFR - prevents reduction of di- to tetra-hydrofolate;
Penetrates CSF, prostate, vaginal fluid;
Res - @ DHFR; |
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Term
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Definition
Anti-Microbial - DNA gyrase - 2nd gen fluoroquinolone;
Dec abs w/ multivalent cations in antacids;
Improved PK;
Inh CTP450;
Res - dec porin proteins, efflux, or binding site axn;
Tx - Hi G- systemic axn, intracellular bacteria;
SE - GI, dizzy, photosens, seizures, crystalluria;
CI - pregnancy, youth |
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Term
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Definition
Anti-Microbial - DNA gyrase - 3rd gen fluoroquinolone;
Dec abs w/ multivalent cations in antacids;
Res - dec porin proteins, efflux, or binding site axn;
Tx - Improved G+ axn, Broad G-, intracellular bacteria;
SE - GI, dizzy, photosens, seizures, crystalluria;
CI - pregnancy, youth |
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Term
| Amphotericin B (Amphocin) |
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Definition
Polyene Antifungal - cell membrane;
Binds ergosterol, forms pore - leak of K,Mg - Cidal efx;
IV admin - hi binding to beta-lipoprotein;
Res - in Candida;
Tx - [deep fungal in preg., systemics] Candida, Crypto, Aspergillus, Blasto;
SE - NEPHROTOX, fever, thrombophlebitis, hypersens, shock/hypoT; |
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Term
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Definition
Antifungal;
Prodrug - inh thymidylate synth - inh DNA synth;
Cidal/static dep. on dose and organism;
Oral admin - Give with AmphB;
Res - dec permease, dec cytosine deaminase (no activation of drug);
Tx - [systemic mycoses] Candida meningitis
SE - hematological, colitis |
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Term
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Definition
Antifungal - cell membrane;
Inh ergosterol synth;
Severe CYP450 inh;
Res - rapid if used alone;
Tx - [broad] Invasive Aspergillus, Scedosporium, Fusarium;
SE - VISUAL DISTURB, PHOTOSENS, HEPATOTOX, teratogenic |
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Term
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Definition
Antifungal - cell membrane;
Inh ergosterol synth;
Mild CYP450 inh;
Res - rapid if used alone;
Tx - [broad] yeasts, dermatophytes, systemic mycoses;
SE - DEC TESTOSTERONE, NO ADRENAL STERIODOGENESIS, teratogenic |
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Term
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Definition
Antifungal;
Inh squalene epoxidase - inh ergosterol synth;
Highly protein bound - Conc in keratin - hair and nails;
Oral or topical admin;
Tx - onychomyosal fungal infxns - nails;
SE - HA, GI, TASTE CHANGES, CHOLESTATIC HEPATITIS |
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Term
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Definition
Antifungal;
Static - disrupts mitotic spindle;
Conc in keratin precursor cells;
CYP450 inducer;
Tx - dermatophytes;
SE - HA, GI, photosens; |
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Term
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Definition
Anti-mycobacterium - cell wall;
Blocks mycolic acid synth - cidal if rapid growth/ static if slow;
Oral admin;
Enters inflamm meninges/CSF, placenta, breastmilk;
Dec efx w/ anatacids, steroids - Met by acetylation;
Res - rapid, use in combo;
Tx - first line for TB;
SE - perhiperal neuropathy, hepatotox, B6 deficiency |
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Term
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Definition
Anti-mycobacterium;
Binds beta subunit of RNApol - cidal to intra/extracellular mycobacteria;
Oral admin - Enters CSF;
CYP450 inducer;
Inc lvls if take w/ probenecid;
Tx - TB (1st line), MRSA, mengingococcus, anti-leprosy;
SE - orange fluids, GI, fever, hepatotox |
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Term
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Definition
Anti-mycobacterium;
Oral admin - Dec abs w/ antacids (Al+++);
Static;
Enters placenta, breastmilk, inflamed meninges/CSF;
Slow resistance;
Tx - first line TB and MAC;
SE - optic neuritis, hyperuricemia, allergic |
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Term
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Definition
Anti-mycobacterium - aminoglycoside;
Targets ribosomes (30S);
IM admin;
Tx - first line TB;
SE - significant toxic profile; |
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Term
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Definition
Herbal supplement - Natural coumarin derivative;
Interaxn w/ Rx anticoagulants |
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Term
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Definition
Herbal supplement;
Contains synephrine, an alpha-1 agonist;
Inh CYP3A4;
SE - stroke, angina, ischemic colitis |
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Term
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Definition
Dietary supplement;
Potent antioxidant;
'Tx' - HTN, ischemic heart disease, prevention of statin-induced myopathy;
SE - poss warfarin interaxn due to VitK-like structure |
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Term
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Definition
Dietary Supplement;
'Tx' to give an Immune boost - no supporting evidence;
Thus antagonizes immunosuppressants;
Induces CYP3A4;
Inhibits CYP1A2 and intestinal 3A4 |
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Term
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Definition
Herbal supplement;
'Tx' - dec cholesterol;
SE - antiplatelet & prolonged bleeding |
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Term
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Definition
Herbal supplement;
'Tx' - preventing AD;
SE - anti-platelet,
Inh CYP1A2 and 2D6 |
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Term
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Definition
Herbal supplement;
Immune boost, CV benefits, dec LDL, dec [glucose];
Thus antagonizes immunosuppressants;
Other SE - prolonged bleeding, inh CYP2D6 |
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Term
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Definition
Herbal supplement - natural coumarin derivative;
Interaxn w/ Rx anticoagulants;
Estrogen-like axns - inc cancer risk |
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Term
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Definition
Herbal supplement;
'Tx' as a laxative;
SE - hepatotox and carcinogenic |
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Term
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Definition
Herbal supplement;
'Tx' - depression (good evidence);
Induces CYP3A4, 1A2, 2C9 |
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Term
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Definition
Mineral supplement;
Imp. cofactor in enzymes, protein and carb metabolism;
Dec childhood diarrhea;
Healing of gastric ulcers;
Tx - sickle cell, acne, ADHD, Down's, herpes, hi cholesterol, plaques and gingivitis |
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Term
Erythropoietin
Note! - Epoetin alpha, darbepoetin alpha |
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Definition
Hematopoietic Growth Factor;
Acts on progenitor cell receptor to inc 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 - cardiotox, nephrotox |
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Term
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Definition
Myeloid Growth Factor;
Stimulates myelopoiesis of granulocytes, etc.;
Tx - severe neutropenia;
SE - granulocyte spike, bone pain, rash |
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Term
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Definition
Myeloid Growth Factor;
Stimulates myelopoiesis of granulocytes, etc.;
Tx - severe neutropenia;
SE - granulocyte spike, bone pain, rash |
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Term
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Definition
Megakaryocyte Growth Factor;
Recombinant IL-11 which inc lymphoid and myeloid growth;
Tx - thrombocytopenia;
SE - fatigue, dizzy, dyspnea, arrhhythmia, edema |
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Term
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Definition
Mineral Iron;
Oral admin;
Tx - DOC for iron deficiency anemia;
SE - heartburn, nausea, GI |
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Term
| Vit B12 (Cyanocobalamin and Hydroxycobalamin) |
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Definition
Vitamin;
Admin parenteral > oral;
Tx - B12 deficiency (megaloblastic - pernicious anemia) |
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Term
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Definition
Vitamin;
Oral or parenteral admin;
Use before preg thru breasfeeding;
Tx - specific deficiency (think prego, chemo, chronic EtOH, upper intestine dz);
Counteracts AED's |
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Term
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Definition
CNS stimulant;
Indirect dopamine agonist - inc BP, wakefulness, alert, concentration, self-confidence, euphoria, physical perform., wt loss;
Psychological dependence;
Tx - obesity, narcolepsy, ADHD;
SE - arrhythmias, angina, HA, abuse (dopamine reward), neurotoxic, convulsions, cerebral hemorrhage, schizo. |
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Term
| Dex-amphetamine (Dexedrine) |
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Definition
CNS stimulant;
Indirect dopamine agonist - inc BP, wakefulness, alert, concentration, self-confidence, euphoria, physical perform., wt loss;
Psychological dependence;
Tx - obesity, narcolepsy, ADHD;
SE - arrhythmias, angina, HA, abuse (dopamine reward), neurotoxic, convulsions, cerebral hemorrhage, schizo. |
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Term
| Methhylphenidate (Concerta) |
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Definition
CNS stimulant - mild;
Indirect dopamine agonist - inc BP, wakefulness, alert, concentration, self-confidence, euphoria, physical perform., wt loss;
Tx - narcolepsy, ADHD;
SE - arrhythmias, angina, HA, abuse (dopamine reward), neurotoxic, convulsions, cerebral hemorrhage, schizo. |
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Term
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Definition
Stimulant;
NE reuptake inh - NE agonist;
Tx - ADHD (esp adults);
Low abuse potential;
SE - anorexia, insomnia, inc HR/BP |
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Term
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Definition
Stimulant;
DA, NE, serotonin reuptake inh;
Tx - obesity (<6 mo. use)
CI - MAOI, anorexia, HTN;
SE - serotonin syndrome, HTN |
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Term
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Definition
Stimulant - unk mech;
No DA effect - no abuse;
Tx - narcolepsy;
Induces CYP450;
SE - HA for 1 week |
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Term
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Definition
Stimulant;
Indirect NE and serotonin agonist;
Tx - short term for obesity;
Low abuse potential;
CI - atherosclerosis, HTN, hyperthyroid, CV dz, MAOIs |
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Term
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Definition
Activates ATIII to inactivate thrombin and factors IX, X, XI, and XII;
Admin SQ or IV;
Variable t1/2 and binding to other plasma proteins - monitor PTT;
Works only for soluble thrombin;
SE - HIT (at 5-10 days); |
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Term
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Definition
Low MW Heparin;
Admin SQ;
Small, long t1/2;
INC anti-Xa axn, Dec plasma protein binding, and dec anti-platelet action;
Tx - DVT prophylaxis;
SE - less potential for HIT (at 5-10 days) |
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Term
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Definition
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 |
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Term
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Definition
Direct Thrombin Inhibitor;
Irreversibly binds active site and exosite 1 of thrombin;
Acts on soluble and CLOT-BOUND THROMBIN;
No immune-med thrombocytopenia;
Source - recombinant form;
Tx - HIT;
SE - (less) hemorrhage;
CI - renal failure |
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Term
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Definition
VitK Antagonist;
Competes w/ Vitamin K epoxide reductase - dec K - Blocks activation of factor II, VII, IX, X - dec thrombin formation;
Slow onset (36-72 hrs), long duration - monitor PT;
Tx - DVT, PE, Afib, Rheumatic heart dz (DOC for the first 3);
SE - skin necrosis, hemorrhage, transient pro-coagulant (inh Protein C), drug interactions (incl. EtOH);
CI - liver disease |
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Term
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Definition
Non-selective COX1/2 IRREV. Inh - anti-platelet;
Acetylation of enzyme;
COX1 inh - no TXA2 - dec aggregation;
COX2 inh - no PGI2 - inc aggregation;
Tx - CHD;
SE - GI bleed, hemorrhagic stroke, asthma;
CI - coumarin, PUD;
Max dose <4g/day |
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Term
| Dipyridamole (Persantine) |
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Definition
PDE Inh - anti-platelet;
Inc cAMP - inh aggregation (prostacyclin-mediated) and inc adenylate cyclase (dec adenosine);
Vasodilator;
Tx - adjunct of aspirin for anti-platelet, adjunct w/ warfarin for prosthetic valves;
SE - HA, dizzy, GI |
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Term
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Definition
ADP Inhibitor - anti-platelet;
Thienopyridine prodrug - activated by CYP2C19 (omeprazole interaxn);
Prevents ADP-GPIIb/IIIa interaction - no platelet activation;
Tx - CHD in higher risk pts (not stable CHD), [2nd line to aspirin] prophylaxis for MI, stroke;
SE - bleeding!;
CI - surgery |
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Term
| Eptifibidate (Integrelin) |
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Definition
GP IIb/IIIa Receptor Block - anti-platelet;
Synthetic;
Prevents binding of fibrinogen or vWF;
IV admin;
Tx - non-Qwave MI, prophylaxis during cardiac cath and angioplasty |
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Term
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Definition
GP IIb/IIIa Receptor Block - anti-platelet;
Monoclonal Ab that targets the receptor;
IV admin;
Tx - prophylaxis during cardiac cath and angioplasty |
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Term
| Streptokinase (Streptase) |
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Definition
1st Gen Thrombolytic;
Forms activator complex with plasminogen;
Non-specific degradation & Streptococcus product = SE's;
Tx - MI, PE, DVT, thrombotic stroke;
SE - systemic lytic state, intracranial hemorrhage, immune response (hypoT, bronchospasm, angioedema, serum sick);
CI - over 75y.o., surgery, HTN, pericarditis; |
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Term
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Definition
2nd Gen Thrombolytic;
Forms tertiary complex w/ fibrin and plasminogen;
SPECIFIC AXN (for fibrin) - local axn;
Tx - MI, PE, or ischemic stroke (w/ no hemorrhage!);
CI - over 75y.o., surgery, HTN, pericarditis; |
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Term
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Definition
3rd Gen Thrombolytic;
r-PA - "small t-PA" (kringle + protease);
Long t1/2;
Admin IV bolus;
SE - inc hemorrhagic stroke;
CI - over 75y.o., surgery, HTN, pericarditis; |
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Term
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Definition
Opiate Anti-diarrheal;
Dec secretions, inc muscle tone (ANTISPASMODIC) incl sphincters (dec urgency @external anal sph), dec motility, inc contact time;
Binds calmodulin;
CI - fever, blood or mucous in stool |
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Term
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Definition
Weak Inhibitor of COX-1,2,(3);
analgesic and antipyretic;
Limited effects on platelets;
NOT useful for anti-inflammatory;
Tx - antipyretic/analgesic for patients taking warfarin or heparin;
SE - HEPATOTOXICITY, stroke, MI;
CI - excessive EtOH, >60y.o.(caution);
Max dose <4g/day |
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Term
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Definition
Expectorant;
Oft combined w/ antihistamines, antitussives |
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Term
| Dimenhydrinate (Dramamine) |
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Definition
1st Gen antihistamine - ether deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma |
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Term
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Definition
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 |
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Term
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Definition
Irreversible Anticholinesterase;
Tx resistant scabies and pediculosis;
Remember: acetylcholinesterase inhibitor (insecticide);
SE - systemic ingestion=cholinergic effects |
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Term
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Definition
Benzodiazepine - balanced anesthesia;
Inc 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) |
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Term
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Definition
Antibiotic;
Give enema to dec colonic bacteria;
Tx - portal HTN, encephalopathy |
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Term
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Definition
Anticholinergic;
Sedation and amnesia;
Pre-op ancillary agent for anesthesia;
Tx reflex bradycardia, block muscarinic anticholinesterases (NM blocker OD);
Drying of secretions;
Blocks pathways from inner ear;
Tx motion sickness |
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Term
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Definition
Beta-1 and 2 antagonist;
direct effect on Na channels, anti-arrythmias;
tx HTN, esp with CHF or prev MI;
SE see BB SEs |
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