Term
Marijuana
(Cannabis sativa) |
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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 |
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Term
| Anandamaide and 2-arachidonylglycerol (2-AG) |
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Definition
Endogenous cannabinoids UPregulated in response to STRESS
Fx: memory plasticity (STM, LTM), regulate cognitive function
Neuroprotective, amnesic, analgesic and inhibit excessive muscle contraction |
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Term
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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 |
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Term
| Cardiovascular effects of Marijuana |
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Definition
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Term
| Immune effects of Marijuana |
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Definition
↓ T-cells; suppress immune response
Via CB2 receptor on lymphocytes and macrophages |
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Term
| Endocrine effects of Marijuana |
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Definition
↓ LH and FSH - ↓ testosterone, testes♂, ↓ libido;
↓GH, ↓ Prl, ↑ACTH;
Anovulatory cycles♀ |
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Term
| Respiratory effects of Marijuana |
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Definition
Acute - bronchodilates;
Chronic - bronchoconstricts |
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Term
| Withdrawl effects of Marijuana |
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Definition
Irritable,
Nausea,
Insomnia,
Sweating,
Anorexia,
Hand tremor,
Restlessness |
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Term
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Definition
| Brain (basal ganglia,cerebellum, hippocampus), adipocytes, liver, duodenum, muscle |
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Term
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Definition
Immune function; pain, neuroinflammation
lymphocytes and macrophages |
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Term
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Definition
Medical marijuana; NATURAL product extracted THC
Approved Use: Antiemetic during chemo, AIDS wasting syndrome;
Possible - MS, spinal injury, Tourette's, dyskinesias |
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Term
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Definition
Medical marijuana; SYNTHETIC cannabinoid
Approved Use: Antiemetic during chemo, AIDS wasting syndrome;
Possible - MS, spinal injury, Tourette's, dyskinesias |
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Term
LSD
(lysergic acid Diethylamide |
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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 |
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Term
Mescaline
3,4,5-trimethoxyphenethylamine |
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Definition
Psychedelic alkaloid, 5HT and DA agonist;
Physio - Sympathomimetic;
Psychic - hallucinations, unusual time perception;
SE - paranoia and fear
Schedule 1 drug |
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Term
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Definition
Cactus known for containing Mescaline
Peyote Buttons |
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Term
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Definition
Substance in Magic Mushrooms;
Physio - sympathomimetic;
Psychic - color, inc laughter, distortions of time/space, hallucinations;
SE - flashback, agitation, panic attacks |
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Term
Psilocin
4-HO-dimethyltryptamine |
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Definition
Dephosphorylated Psilocybin - Substance in Magic Mushrooms;
Physio - sympathomimetic;
Psychic - color, inc laughter, distortions of time/space, hallucinations;
SE - flashback, agitation, panic attacks |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
Salvia Divinorum
(Salvinorin A) |
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
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Definition
Cough suppressant; Robotripping
NMDA receptor antagonist;
Dissociative anesthetic |
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Term
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Definition
Dramamine;
anticholinergic;
Tx motion sickness;
Abuse - disorientation, delirium, amnesia and delusions |
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Term
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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 |
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Term
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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 |
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Term
| Smokeless tobacco (Types) |
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Definition
Snuff - European dry tobacco, inhaled;
Dip/'snuff' - American moist, mouth;
Snus - Scandanavian moist, mouth, powder |
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Term
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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 |
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Term
| Nicotine Patch (Habitrol) |
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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 |
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Term
| Nicotine inhaler (Nicotrol) |
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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 |
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Term
| Low- or no-nicotine cigarettes (Eclipse) |
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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; |
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Term
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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! |
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Term
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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 |
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Term
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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 |
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Term
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Definition
TCA - Non-nicotine cessation aid;
Lipophilic - cross BBB;
Long t1/2 16-90; hepatic metabolism CYP2D6
High efficacy in depressed pts; |
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Term
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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 |
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Term
| Ethanol CNS damage, mechanisms |
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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 |
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Term
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Definition
Early: agitation, confusion, hyperactive ANS, seizure(2-48hrs)
Late: Delirium Tremons- hyperthermia, hallucination, disorientation;
Coma, death
Trx: BNZ, phenytoin, Phenobarbital (siezures) atenolol, clonidine |
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Term
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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 |
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Term
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Definition
Rubbing alcohol;
Oxidized to form acetone(!); slower than EtOH
SE - inc CNS tox, severe gastritis, nausea, pain;
Tx OD w/ hemodialysis |
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Term
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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 |
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Term
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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 |
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Term
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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' |
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Term
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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; |
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Term
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Definition
Anti-emetic - 5-HT3 antagonist;
Dec craving by blocking the reward pathway;
Tx - chronic alcoholism; |
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Term
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Definition
AMPA-R antagonist, GABA-R regulator;
Tx - chronic alcoholism;
Dec 'heavy drinking days';
Need to titrate dosing;
SE – glaucoma |
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Term
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Definition
Tx EtOH withdrawal stages...
Tremulousness syndrome,
Seizures,
DT |
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Term
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Definition
Tx EtOH withdrawal stages...
tremulousness syndrome,
DT |
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Term
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Definition
Tx EtOH withdrawal stages...
seizures |
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Term
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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; |
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Term
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Definition
Benzodiazepine antagonist;
Tx BNZ OD;
Can produce withdrawal symptoms, not used too often;
SE - N/V, dizzy, panic attacks, seizures, blurred vision |
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Term
| Digoxin Immune Fab (Digibind) |
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Definition
Ig against digoxin/digitalis;
Tx digoxin OD;
Corrects hyperkalemia;
Inc total serum [digoxin] due to redistribution from tissues |
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Term
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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 |
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Term
| Physostigmine (Antilirium) |
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Definition
reversible anticholinesterase;
tx atropine O.D., other anticholinergic (antidepressant, antihistamine, antiemetic, antipsychotics) OD
crosses BBB, CNS stim then depression;
CI - TCA's |
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Term
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Definition
reversible anticholinesterase;
tx ANTICHOLINERGIC OD;
can reverse non-depol NM blockers |
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Term
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Definition
| Tx gas intoxication by irrtants such as chlorine, ammonia, sulfur dioxide |
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Term
| Cyanide kit (Na nitrate + thiosulfate) |
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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 |
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Term
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Definition
Tx organophoshate (insecticide) OD;
Use with supportive tx |
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Term
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Definition
reactivator of cholinesterase;
Slow IV admin;
Tx organophosphate, sarin, soman OD!;
Rapid admin SE's - NM block, msucle spasm, HTN, tachycardia |
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Term
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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 |
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Term
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Definition
Chelator;
First line tx for arsenic poisoning;
Also Tx lead, mercury poisoning;
SE - nephrotoxic;
CI - G6PD deficiency |
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Term
| Penicillamine (Cuprimine) |
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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 |
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Term
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Definition
Iron chelator;
Tx - first line for iron tox;
SE - red urine, tachycardia, hypoT, abdominal pain, N/V, flush, fever |
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Term
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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; |
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Term
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Definition
| Rattlesnake antivenom via SMALL Ab fragments (dec immune response) |
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Term
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Definition
Used in high risk black widow spider bites;
Questionable benefit in brown recluse;
SE - hypersensitivity based on source, coagulopathies |
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Term
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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) |
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Term
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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
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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
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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 |
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Term
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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 |
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Term
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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
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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 |
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Term
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Definition
Atypical antidepressant;
MOST POTENT SNRI; 100X > venlafaxine
CYP2D6 1A2 metabolism; t1/2=12 hrs
95% protein bound; |
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Term
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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) |
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Term
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Definition
Atypical antidepressant; 2nd Generation
NE reuptake inhibitor (NRI); NO 5HT activity
SE –↑ SEIZURE risk |
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Term
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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
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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 |
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Term
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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 |
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Term
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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! |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
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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 |
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Term
| Tranylcypromine (Parnate) |
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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
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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
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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
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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
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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) |
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Term
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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 |
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Term
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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; |
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Term
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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; |
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Term
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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; |
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Term
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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; |
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Term
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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 |
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Term
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Definition
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Term
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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; |
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Term
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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 |
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Term
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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; |
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Term
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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 |
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Term
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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 |
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Term
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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) |
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Term
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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 |
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Term
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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) |
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Term
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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 |
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Term
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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 |
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Term
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Definition
| Attenuation of SCN activity, induces sleep |
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Term
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Definition
| Maintenance of circadian rhythm |
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Term
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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 |
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Term
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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 (?) |
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Term
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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 |
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