Shared Flashcard Set

Details

Assessment 11
Pharm - Drugs of Abuse, Toxicology, Anti-depressants, Sedative/hypnotics
122
Pharmacology
Professional
01/03/2011

Additional Pharmacology Flashcards

 


 

Cards

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
Anandamaide and 2-arachidonylglycerol (2-AG)
Definition
Endogenous cannabinoids UPregulated in response to STRESS

Fx: memory plasticity (STM, LTM), regulate cognitive function
Neuroprotective, amnesic, analgesic and inhibit excessive muscle contraction
Term
CNS effects of Marijuana
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
Inc HR - bloodshot eyes
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
CB1 receptors
Definition
Brain (basal ganglia,cerebellum, hippocampus), adipocytes, liver, duodenum, muscle
Term
CB2 receptors
Definition
Immune function; pain, neuroinflammation
lymphocytes and macrophages
Term
Dronabinol (Marinol)
Definition
Medical marijuana; NATURAL product extracted THC
Approved Use: Antiemetic during chemo, AIDS wasting syndrome;
Possible - MS, spinal injury, Tourette's, dyskinesias
Term
Nabilone (Cesamet)
Definition
Medical marijuana; SYNTHETIC cannabinoid
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
Peyote
Definition
Cactus known for containing Mescaline
Peyote Buttons
Term
Psilocybin
Definition
Substance in Magic Mushrooms;
Physio - sympathomimetic;
Psychic - color, inc laughter, distortions of time/space, hallucinations;
SE - flashback, agitation, panic attacks
Term
Psilocin
4-HO-dimethyltryptamine
Definition
Dephosphorylated Psilocybin - Substance in Magic Mushrooms;
Physio - sympathomimetic;
Psychic - color, inc laughter, distortions of time/space, hallucinations;
SE - flashback, agitation, panic attacks
Term
Phencyclidine
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
MDMA
Definition
Ecstasy - blocks NT reuptake at synapse - dopaminergic and serotonergic;
Physio - inc BP HR, dry mouth, bruxism;
CNS - euphoria, "loving feeling," inc intimacy, loss of boundaries, dec inhibition, dec defenxe;
Cognitive - slowed thoughts; impaired form and content
Perceptual - visual hallucinations, altered time/space, spatial
AE: chronic-atrophy ↓5HT and DA neurons and transporters
Term
Cathione (Khat)
Definition
Monoamine alkaloid, found in the shrub Catha edulis (khat)
Similar to ephedrine and other amphetamines, Schedule 1 drug
MOA: Release of DA
Physical - HTN, ↑ HR, arrhythmia, MI, vasoconstrict;
CNS: insomnia, cerebral hemorrhage;
Psychic - hallucinations, mania, hypomania, euphoria, aggressive, anxiety, emotionally unstable, inc imagination, schizo
Term
Salvia Divinorum
(Salvinorin A)
Definition
Member of mint family (Sally G, Magic mint)
Sort acting CNS effects, disassociated from self, solitary
AE: Sometimes fearful
Think ketamine like and Miley Cyrus
Term
Volatile Solvents
Definition
Paint thinner, dry-cleaning, glue, markers, gasoline, degreasers, shoe polish, toluene
Acute: activation of dopamine - CNS depressant;
Slurred speech, ataxia, euphoria, dizzy, hallucinations, delusions;
SE - demyelination neurotoxicity, ataxia, ↓ lymphocytes, ↓ NK cell
Organotoxic, teratogenic, AIDS progression
Sudden sniffing death, cardiac arrhythmias; COD-choking, suffocation, asphyxiation
Term
Aerosols
Definition
spray paint, veggie spray, deodorant, hair spray;
Acute: activation of dopamine - CNS depressant;
Slurred speech, ataxia, euphoria, dizzy, hallucinations, delusions;
SE - demyelination neurotoxicity, ataxia, ↓ lymphocytes, ↓ NK cell
Organotoxic, teratogenic, AIDS progression
Sudden sniffing death, cardiac arrhythmias; COD-choking, suffocation, asphyxiation, Fatal injury
Term
Gases
Definition
Ether, chloroform, NO, halothane, butane, propane;
Acute: activation of dopamine - CNS depressant;
Slurred speech, ataxia, euphoria, dizzy, hallucinations, delusions;
SE - demyelination neurotoxicity, ataxia, ↓ lymphocytes, ↓ NK cell
Organotoxic, teratogenic, AIDS progression
Sudden sniffing death, cardiac arrhythmias; COD-choking, suffocation, asphyxiation
Rapid uptake in highly perfused organs, lung brain, kidney
Term
Nitrates
Definition
Cyclohexyl nitrate, isoamylnitrate, isobutyl nitrate, video head cleaner, room deodorizer,Sexual enhancers, "poppers and snappers";
Acute: activation of dopamine - CNS depressant;
Slurred speech, ataxia, euphoria, dizzy, hallucinations, delusions;
SE - demyelination neurotoxicity, ataxia, ↓ lymphocytes, ↓ NK cell
Organotoxic, teratogenic, AIDS progression
Sudden sniffing death, cardiac arrhythmias; COD-choking, suffocation, asphyxiation interacts cialis, viagra
Term
Dextromethorphan
Definition
Cough suppressant; Robotripping
NMDA receptor antagonist;
Dissociative anesthetic
Term
Dimenhydrinate
Definition
Dramamine;
anticholinergic;
Tx motion sickness;
Abuse - disorientation, delirium, amnesia and delusions
Term
Nicotine
Definition
Acts on variety of nicotinic receptors (pentameric, ligand-gated) in different locations and composed of combinations of subunits α 2-9, β 2-4;
High rates of dependence, physical withdrawal severity ranks b/t heroin and cocaine
Term
Cigarette tobacco
Definition
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
Term
Smokeless tobacco (Types)
Definition
Snuff - European dry tobacco, inhaled;
Dip/'snuff' - American moist, mouth;
Snus - Scandanavian moist, mouth, powder
Term
Nicotine gum (Nicorette)
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
Nicotine inhaler (Nicotrol)
Definition
Inhaler and spray25% abs @ 3 mo.;
Limited efficacy after 3 mos based on behavioral disruption;
Best efficacy in combination with cessation programs;
SE - [spray] nasal irritation, [inhaler] mouth and throat irritation;
CI - chronic rhinitis, active smoking additive
Term
Low- or no-nicotine cigarettes (Eclipse)
Definition
↓ exposure to toxins by heating tobacco w/out burning it;
↓ use and effectiveness due to complexity of drug delivery device, lack of taste and image
CI - active smoking additive
Basically ineffective, other products Quest, Accord
Term
Smokeless tobacco
Definition
Insert under lip;
Maintain low plasma [nicotine] ad libitum
'Snus' form has ↓incidence of oral cancer (pasteurized instead of fermented);
Chew or dip is fermented tobacco, American, Skoal, Redman
CI - active smoking additive
Term
Buproprion (Zyban)
Definition
Antidepressant, non-nicotine cessation aid
MOA unk, but somehow linked to NE and DA possible
60% abs @ 9 wks
24% abs @ 1 yr;
Enhances efficacy of other tx/Rx e.g nicotine based;
Well tolerated, low abuse potential;
SE – Metabolized by CYP2D6; drug interactions
CI - seizures, anorexia, bullemia, BB warning suicidal ideation
Term
Varenicline (Chantix)
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
Mecamylamine
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
Rimonabant (Acomplia)
Definition
Non-nicotine cessation aid; CB1 anTagonist;
Anti-obesity in Europe + reduce wt gain during smoking cessation;
Effective short term; 2nd line tx;
SE - SEVERE depression!
Term
Nic VAX
Definition
Non-nicotine cessation aid; a nicotine conjugate vaccine
Abs produced to trap nicotine in plasma, can't activate reward pathways in brain;↓nicotine related release of DA in nucleus accumbens
Short term use - either to initiate quitting or prevent relapse
16% remain quit at 12 months
Term
Clonidine (Catapres)
Definition
Non-nicotine cessation aid, anti-HTN;
Crosses BBB t1/2=1.3 hrs
Direct acting alpha2 agonist in medulla, ↓sym outflow;
Can admin as transdermal patch; 2nd line cessation tx;
Tx EtOH withdrawal stages...
AE: Tremulousness syndrome, sedation
Term
Nortriptyline (Aventyl)
Definition
TCA - Non-nicotine cessation aid;
Lipophilic - cross BBB;
Long t1/2 16-90; hepatic metabolism CYP2D6
High efficacy in depressed pts;
Term
Ethanol
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
Ethanol withdrawal
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
Methanol
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
Isopropanol
Definition
Rubbing alcohol;
Oxidized to form acetone(!); slower than EtOH
SE - inc CNS tox, severe gastritis, nausea, pain;
Tx OD w/ hemodialysis
Term
Thiamine
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
Disulfiram (Antabuse)
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
Naltrexone (ReVia)
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
Acamprosate (Campral)
Definition
NMDA receptor antagonist and mGlu R5 modulator;
Dec EtOH relapses;
Tx - chronic alcoholism;↓cravings, ↓negative effects
SE - nervousness, fatigue, diarrhea;
REDUCE dose w/ renal insufficiency;
Term
Ondasetron (Zofran)
Definition
Anti-emetic - 5-HT3 antagonist;
Dec craving by blocking the reward pathway;
Tx - chronic alcoholism;
Term
Topiramate (Topamax)
Definition
AMPA-R antagonist, GABA-R regulator;
Tx - chronic alcoholism;
Dec 'heavy drinking days';
Need to titrate dosing;
SE – glaucoma
Term
Benzodiazepines
Definition
Tx EtOH withdrawal stages...
Tremulousness syndrome,
Seizures,
DT
Term
Atenolol (Tenormin)
Definition
Tx EtOH withdrawal stages...
tremulousness syndrome,
DT
Term
Phenytoin (Dilantin)
Definition
Tx EtOH withdrawal stages...
seizures
Term
N-acetylcysteine, NAC
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
Flumazenil (Romazicon)
Definition
Benzodiazepine antagonist;
Tx BNZ OD;
Can produce withdrawal symptoms, not used too often;
SE - N/V, dizzy, panic attacks, seizures, blurred vision
Term
Digoxin Immune Fab (Digibind)
Definition
Ig against digoxin/digitalis;
Tx digoxin OD;
Corrects hyperkalemia;
Inc total serum [digoxin] due to redistribution from tissues
Term
Naloxone (Narcan)
Definition
opioid receptor antagonist;
IV only: rapid onset, short duration (esp compared to morhphine), dose accordingly;
EXTENSIVE P.O. FIRST PASS METABOLISM;
tx opioid OD, reverses respiratory depression;
can cause opioid withdrawal; start low, go slow
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
Neostigmine (Prostigmin)
Definition
reversible anticholinesterase;
tx ANTICHOLINERGIC OD;
can reverse non-depol NM blockers
Term
O2 + Bronchodilators
Definition
Tx gas intoxication by irrtants such as chlorine, ammonia, sulfur dioxide
Term
Cyanide kit (Na nitrate + thiosulfate)
Definition
Na nitrate + thiosulfate + amyl nitrate;
[1] Inhale amyl nitrate;
[2] IV Na Nitrate - conv hemoglobin to methemoglobin (affinity for CN);
[3] Na thiosulfate - conv (cyan)methemoglobin to thiocynate for renal elimination (hemoglobin released!);

BUT ... not effective in given timeline
Term
Atropine
Definition
Tx organophoshate (insecticide) OD;
Use with supportive tx
Term
Pralidoxime (2PAM)
Definition
reactivator of cholinesterase;
Slow IV admin;
Tx organophosphate, sarin, soman OD!;
Rapid admin SE's - NM block, msucle spasm, HTN, tachycardia
Term
Succimer (Chemet, DMSA)
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
Dimercaprol
Definition
Chelator;
First line tx for arsenic poisoning;
Also Tx lead, mercury poisoning;
SE - nephrotoxic;
CI - G6PD deficiency
Term
Penicillamine (Cuprimine)
Definition
Chelator;
Tx - copper, iron, lead, and mercury tox; 2nd line for aresenic poisoning;
Also used in RA, wilson's dz;
SE - anemias, thrombocytopenia, agranulocytosis, renal fail, tinnitus, neuropathy, ON, agitation, dystonia etc...
Dec use due to many SE's
Term
Deferoxamine (Desferal)
Definition
Iron chelator;
Tx - first line for iron tox;
SE - red urine, tachycardia, hypoT, abdominal pain, N/V, flush, fever
Term
Deferasirox (Exjade)
Definition
Iron chelator;
Tablet dissolved in liquid;
Tx - chronic iron tox due to blood transfusions;
SE - nausea, abdominal pain, HA, pyrexia, cough, inc [creatinine] and [hepatic enzymes], audio/visual disturbance;
Term
CroFAB antivenom
Definition
Rattlesnake antivenom via SMALL Ab fragments (dec immune response)
Term
Antivenom
Definition
Used in high risk black widow spider bites;
Questionable benefit in brown recluse;
SE - hypersensitivity based on source, coagulopathies
Term
Amitriptyline (Elavil)
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
Imipramine (Tofranil)
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
Term
Nortriptyline (Pamelor)
Definition
TCA (secondary amine) ACTIVE METABOLITE - inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation; POTENT 5HT, less sedating than amitrtiptyline
Blocks mAch, 5-HT, and histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility;
Low therapeutic index;
SE - orthostatic hypoT, tachycardia, confusion, dry mouth, constipation, urinary retention, sedation, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine
Term
Clomipramine (Anafranil)
Definition
TCA - inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation; metabolite MORE strongly NE inhibitor
Blocks mAch, 5-HT, and histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility; Low therapeutic index; CYP1A2 metabolism
SE - orthostatic hypoT, tachycardia, confusion, dry mouth, constipation, urinary retention, sedation, worsen narrow-angle glaucoma and CHF, acidosis, delirium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine
Term
Protriptyline (Vivactil)
Definition
TCA - 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;
SE - orthostatic hypoT, tachycardia, confusion, dry mouth, constipation, urinary retention, sedation, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine
Term
Despiramine (Norpramin)
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)
Term
Trimipramine (Surmontil)
Definition
TCA - 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;
SE - orthostatic hypoT, tachycardia, confusion, dry mouth, constipation, urinary retention, sedation, worsen narrow-angle glaucoma and CHF, acidosis, delerium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine
Term
Doxepin (Sinequan)
Definition
TCA - inhibits reuptake of NE and 5-HT at presynaptic terminals = potentiation;
Blocks mAch (ANTICHOLINERGIC), 5-HT, and (SEDATING) histamine receptors;
Tx - depression, anxiety, ADHD, nocturnal enuresis;
High lipid solubility; Low therapeutic index;
SE - orthostatic hypoT, tachycardia, confusion, dry mouth, constipation, urinary retention, sedation, worsen narrow-angle glaucoma and CHF, acidosis, delirium, seizures;
CI: Additive CNS depression (EtOH, hypnotics) ↓effect of anti-HTN clonidine, methyl-DOPA and guanethidine
Term
Bupropion (Wellbutrin)
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
Term
Venlafaxine (Effexor)
Definition
Atypical antidepressant; 3rd Generation
Serotonin and NE reuptake inhibitor (SNRI); NO SEDATION, NO anticholinergic, NO adrenergic
Short t1/2; 4-10 hrs
SE - mild HTN, sweating, dizzy, nausea, anxiety
Term
Duloxetine (Cymbalta)
Definition
Atypical antidepressant;
MOST POTENT SNRI; 100X > venlafaxine
CYP2D6 1A2 metabolism; t1/2=12 hrs
95% protein bound;
Term
Amoxapine
Definition
Atypical antidepressant; 2nd Generation
Mixed inhibition of NET>SERT~DAT;
Analog of loxapine - use for depression in psychotic pts;
SE - extrapyramidal motor effects (some DA antagonism)
Term
Maprotiline (Ludiomil)
Definition
Atypical antidepressant; 2nd Generation
NE reuptake inhibitor (NRI); NO 5HT activity
SE –↑ SEIZURE risk
Term
Mirtazepine (Remeron)
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;
Term
Trazodone (Desyrel)
Definition
Atypical antidepressant; 2nd Generation
5-HT reuptake inhibitor; VERY SEDATING t1/2=2-9 hrs
Tx depression w/ sleep disturbance and/or anxiety;
CI: INHIBITS CYP3A4
Term
Nefazodone
Definition
Atypical antidepressant; 3rd Generation POTENT anticholinergic
5-HT reuptake inhibitor; NO NE effect, t1/2=2-4 hrs
Tx depression w/ sleep disturbance and/or anxiety;
CI: INHIIBITS CYP3A4
Term
Citalopram (Celexa)
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
First line Trx for MDD< panic attack, OCD, ADHD ….
Long t1/2 - 3 days; High therapeutic index;
SE - nausea, dec libido; LEAST side effects of SSRI
CI - MAOI, amphetamines, ecstasy, LSD, L-tryptophan;
Serotonin syndrome!
Term
Fluoxetine (Prozac)
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
Long t1/2 - a WEEK!; METABOLITE norfluoxetine t1/2 = 7-9 d
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
Term
Paroxetine (Paxil)
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
Long t1/2 - 1-4 days;
High therapeutic index;
SE - nausea, ↓libido, TERATOGEN;
CI - MAOI, amphetamines, LSD, L-tryptophan;
Serotonin syndrome!
MAY ↑levels of theophylline, warfarin, procyclidine and TCA
Term
Sertraline (Zoloft)
Definition
SSRI - inhibits SERT to potentiate serotonin action;
CNS stimulation, euphoria;
Long t1/2 = 1-4 days; High therapeutic index;
SE - nausea, ↓ libido;
CI - MAOI, amphetamines, LSD, L-tryptophan;
Serotonin syndrome!
MAY ↑effects warfarin, and TCA
Term
Fluvoxamine (Luvox)
Definition
SSRI - inhibits SERT to potentiate serotonin axn;
CNS stimulation, euphoria;\00000
Long t1/2 - 1-4 days;
High therapeutic index;
SE - nausea, ↓ libido;
CI - MAOI, amphetamines, LSD, L-tryptophan;
Serotonin syndrome!
MAY ↑levels of theophylline, warfarin, alprazolam and TCA
Term
Serotonin Syndrome
Definition
SSRI + MAOI, Ecstasy, TCA.dextropmethorphan, meperidine, St. John’s Wort
Overstimulation of 5-HT1A in midbrain the central grey and medulla;
Hyperthermia, hyperreflexia, tremor, myoclonus, agitation, seizures, confusion, delirium, CV collapse, coma, death
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
Term
Isocarboxazid (Marplan)
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
Term
Phenelzine (Nardil)
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
Term
Lithium (Lithobid)
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
Term
Valproate (Depacon)
Definition
Mood-stabilizer and anti-convulsant;
Inhibits voltage-gated Na channels @ inactivated state;
Blocks Ca channels, ↓NT release by vesicles
Stimulate GABA synthesis and inhibits degradation;
Displaces phenytoin from plasma proteins;
SE - nausea, abdominal pain, heartburn, sedation, hepatotoxicity (MUST MONITOR LIVER enzymes)
CI: Inhibits its own metabolism and others, interacts with carbamazepine and amitriptyline, ↓folate (birth defects)
Term
Carbamazepine (Tegretol)
Definition
Mood-stabilizer and anti-convulsant;
DOC partial seizures and trigeminal neuralgia;
Inhibits Na channels (prolonged channel recovery and ↓neural AP);
Poor solubility, distributes slowly;
Metabolized by CYP3A4, [INDUCES] CYP 2C and CYP3A, UDP-glucuronyl transferase families;
T1/2 - 36 hrs;
SE - diplopia, ataxia, rash, aplastic anemia, effects [Oral Contraceptive] activity
Term
Estazolam (ProSom)
Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left); Require GABA;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates; t1/2 = 19 hr
Drug-drug interactions at CYP-P450 3A4 Ritonavir
Pregnancy category X, schedule IV;
Term
Flurazepam (Dalmane)
Definition
BNZ - approved for insomnia; NOT preferred up to 4 days in system
Modify the response of GABA receptor to GABA (shift dose response curve left);Require GABA ;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates; t1/2 = 40-250 hrs
Drug-drug interactions at CYP-P450 3A4
METABOLIC ACCUMULATION
Cross TOLERANCE with opiods
Pregnancy category X, schedule IV;
Term
Quazepam (Doral)
Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left); Require GABA; SELECTIVE GABA type 1
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates; t1/2 = 27-41 hrs
Drug-drug interactions at CYP-P450 32B6 some 3A4
METABOLIC ACCUMULATION, less tolerance
Pregnancy category X, schedule IV;
Term
Temazepam (Restoril)
Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);Require GABA;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment; Direct conjugation 80% renal, 20 % hepatic, t1/2 = 3.5-18 hrs
[NO P450 INTERACTIONS]
Drug-drug interactions at CYP-P450s
Pregnancy category X, schedule IV;
Term
Triazolam (Halcion)
Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left); Require GABA;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Drug-drug interactions at CYP-P450 3A4
RAPIDLY ELIMINATED, tolerance, t1/2 = 2-4 hrs
Pregnancy category X, schedule IV;
Serial Killer Jeffrey Dahmer’s DOC for his victims
Term
BZ-1 receptor
(2 actions)
Definition
sedation;
amnesia
Term
Zolpidem (Ambien)
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;
No clinically crucial lethality; t1/2 = 2-3 hrs
Pregnancy category C (Okay, but caution), schedule IV;
Term
Zaleplon (Sonata)
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;
No clinically crucial lethality; t1’2 = 1 hr
Pregnancy category C (Okay, but caution), schedule IV;
ETHNIC VARIABILITY - Asians, must ↓ the dose ALDH
Term
Eszopiclone (Lunesta)
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;
No clinically crucial lethality; t1/2 = 6 hrs
Pregnancy category C (Okay, but caution), schedule IV;
Term
Flumazenil (Romazicon)
Definition
BNZ and BRA antagonist !;
Reversal of sedation or overdose; Extremely SHORT half life, initial t1/2 =15 min, Brain 20-30 min terminal ~80 minutes
IV admin- short duration calls for re-dose to cover the longer-acting BNZs;
Effects: Abrupt awakening, dysphoria, agitation;
DOES NOT reverse effects of barbiturates, opiate agonists, TCAs
Term
Amobarbital (Amytal)
Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM
Term
Aprobarbital (Alurate)
Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
(NO extensive HEPATIC metabolism)
Term
Pentobarbital (Nembutal)
Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM
Term
Phenobarbital (Luminal)
Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria,
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
(NO extensive HEPATIC metabolism)
Term
Secobarbital (Seconal)
Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM
Term
Ramelteon (Rozerem)
Definition
Melatonin receptor agonist; MT1 and MT2 (No MT3 activity)
Not a schedule drug;
No residual effects (morning after);
Drug interactions with substrates of CYP1A2 (2C9, 3A4);
No metabolic accumulation;
Adverse effects - HA, nausea, URI, Somnolence, PROLACTINEMIA insomnia (paradox);
Pregnancy C
Higher specificity than melatonin,
↓ dose: longer t1/2 = ~2.6 hrs
Term
MT1 receptor binding
Definition
Attenuation of SCN activity, induces sleep
Term
MT2 receptor binding
Definition
Maintenance of circadian rhythm
Term
Quietiapine (Seroquel)
Definition
Antipsychotic used for off-label insomnia;
MOA – sedation via H1 receptors; antagonist 5HT, DA, α1-2
SE - QT prolongation, orthostatic hypotension, weight gain, constipation, xerostomia
Term
Gabapentin (Neurontin)
Definition
Anticonvulsant used for off-label insomnia; neuropathic pain and MDD
Unknown mechanism; not GABA, not Na channel blocker;
SE - Fatigue, weight gain, dizziness, ataxia, nystagmus,
SUICIDAL IDEATION (?)
Term
Diphenhydramine
Definition
Benadryl, 1st Generation antihistamine;
cross BBB for H1 antagonism;
SE - Xerostomia, blurred vision, urinary retention, inc intraocular pressure (think glaucoma!);
Rapid tolerance with rebound insomnia;
Caution in elderly
Supporting users have an ad free experience!