Non-medical drugs Flashcards
Fomepizole (Antizol)
Mech: Blocks alcohol dehydrogenase
Thera: Methanol & ethylene glycol poisoning
Misc: Very expensive;
INSTEAD use ethyl alcohol (vodka) to deal with both poisoining types and prevent acidosis and nephrotoxicity from ethylene glycol (through oxalic acid) and severe acidosis and retinal damage from methanol (through formaldehyde and formic acid)
Cocaine
Class: CNS stimulant
Mech: Blocks reuptake of dopamine, norepinephrine, and serotonin
Thera: Topical anesthetic, combined vasoconstrictor and local anesthetic
Important SE’s: Sympathetic effects; paranoia, aggression, euphoria, disinhibited, hyperactive
Misc: Rapidly hydrolyzed by plasma cholinesterase with some backdown by P450 and spontaneous hydrolysis; crack is the free base form; the metabolite benzoylecgonine in urine tells you there’s cocaine in system
LSD
Class: Schedule I Hallucinogen
Mech: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory and emotional input; partial dopamine agonist
Thera: Schedule I hallucinogen; model hallucinogen against which all others compared; limited studies in psychoanalysis, alcoholism, autistic children, and terminal cancer patients
Important SE’s: Bad trips (anxiety attack, panic attack), flashbacks, “street drug” lifestyle; no overdoses, birth defects, or chronic psychoses linked to LSD
Misc: Oxidized in liver; cross tolerance with mescaline and psilocybin; could need to TALK DOWN patient during the bad trips and maybe diazepam!!!
Mescaline
Class: Schedule I Hallucinogen
Mech: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory input; partial dopamine agonist
Misc: Cross tolerance with LSD and psilocybin
Psilocybin
Class: Schedule I Hallucinogen
Mech: Agonist at 5HT2A receptors on Raphe cell body –> inhibition of Raphe Nuclei firing –> increased sensory input; partial dopamine agonist
Misc: Cross tolerance with mescaline and LSD
Phencyclidine (PCP)
Class: Dissociative anesthetic
Mech: Antagonist of ion channel associated with NDMA receptor; agonist at mu opioid receptors
Important SE’s: Violent behavior, coma, seizures, arrest; inexplicable psychoses
Other SE’s: Dissociation, confusion, ataxia, marked nystagmus
Misc: Long half-life due to being highly lipid soluble and having active metabolites; treat with isolation and a diazepam and sometimes anti-psychotic
Amphetamines (Benzadrine)
Mech: Indirect sympathomimetic (release biologic amines from nerve terminals in periphery and in CNS); dopamine most important
Thera: Narcolepsy, ADHD
Important SE’s: Vasospasm leading to possible stroke or MI, arrhythmia, weight loss (anorectic effect)
Other SE’s: Tremor, anxiety, irritability, confusion, possibly paranoid state
Misc: Others: dextroamphetamine (Dexedrine), methamphetamine (Desoxyn), methylphenidate (Ritalin)
Marijuana (THC)
Class: Cannabinoid
Mech: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
Thera: Schedule I hallucinogen; anti-emetic, anti-nausea, and appetite stimulate for cancer chemotherapy and AIDS patients; analgesic for neuropathic pain; potentially: glaucoma, asthma, anxiolytic, migraine, and multiple sclerosis treatment
Important SE’s: Vasodilation –> tachycardia, dilation of conjunctival vessels, bronchodilation, decreased intraocular pressure, hunger; euphoria, heightened sensory awareness, sedation
Other SE’s: May impair reproductive function in adolescents; heavy use may impair development and learning of very young users; possible respiratory damage due to tar;
Misc: Active ingredient is delta-9-tetrahydrocannabinol; metabolized by P450, with chronic use inducing enzyme; highly lipid soluble
Anandamide
Class: Endogenous cannabinoid
Mech: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
Thera: Endogenous cannabinoid
Dronabinol (Marinol)
Class: Synthetic THC
Mech: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
Thera: Schedule III drug; anti-emetic, anti-nausea, and appetite stimulate for cancer chemotherapy and AIDS patients
Nabilone (Cesamet)
Class; Synthetic THC
Mech: Hits cannabinoid receptors (CB1, CB2: G-protein coupled receptors)
Thera: Schedule II drug; treatment-resistant nausea and vomiting, weight loss and anorexia in AIDS patients
Misc: Less psychoactive side effects than marijuana
Alcohol: rate of absorption, distribution, elimination:
- rate of absorption: rapidly absorbed by diffusion through membranes; crosses mostly at small intestine; rate depends on concentration of alcoholic beverage and if stomach is empty or full (with meal, you get peak BAC at later time than with empty stomach, and AUC is lower WITH MEAL!!);
food in stomach delays stomach emptying, dilutes alchol, increases effective rate of alcohol metabolism - Distribution: it is the TBW, such that males have more body water and body fat content than females on average
- Elimination: metabolism in LIVER mostly; some in stomach; eliminated through urine, breath, sweat;
need Alcohol DH (beta 2 allele enhances hepatic conversion of EtOH to acetaldehyde, elevating blood concentration of acetaldehyde; also if you also lack ALDH2 in liver mito, you can get elevated acetaldehyde levels leading to facial flushing, dizziness, nausea, increased pulse rate); all NAD-dependent reactions in liver affected by alcohol;
mech of elimination is ZERO ORDER KINETICS
Most sensitive area for alcohol? Least sens?
- Frontal lobe (removal of inhibitions)
2. Medulla (decreased respiration and temp and potentially death)
Consequences of alcohol metabolism on liver:
Think fatty liver, then hepatitis, necrosis, fibrosis, cirrhosis, hepatic failure, death
Alcohol can raise ____ and protect against ____ at:
HDL levels; CHD;
lower levels, but you get J- or U-shaped curve with alcohol consumption above 1 drink/day with mortality rising with increasing dose
