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106 Cards in this Set
- Front
- Back
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Acetylcholine
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Neurotransmitters in the CNS
acts on M and N receptors; memory, cognition, attention; Ach neurons degenerate in Alzheimer’s; balances out DA |
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Norepinephrine
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Neurotransmitters in the CNS
↓ = depression; pain regulation |
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Dopamine
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Neurotransmitters in the CNS
addiction, emotions, movement; Nigro-striatal DA neuron degeneration in Parkinson’s; excess = psychosis, schizophrenia |
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Serotonin (5-HT
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Neurotransmitters in the CNS
decrease=depression, anxiety; excess = sleep; raphe nuc to limbic |
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GABA
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Neurotransmitters in the CNS
major inhibitory, interneurons; ↑=anxiety relief; ↓ = seizures (↑NMDA activity) GABAA - ↑Cl conductance GABAB - ↑K, ↓Ca conductance |
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Glutamate
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Neurotransmitters in the CNS
major excitatory; inotropic, metabotropic; etoh blocks @ NMDA; NMDA receptor – learning, memory, long term potentiation; ↑ = seizures |
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Glycine
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Neurotransmitters in the CNS
inhibitory; brain stem & spinal cord interneurons; blocked by strychnine |
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Neuropeptides
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Neurotransmitters in the CNS
endogenous opiates; endorphins, enkephalin, substance P |
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Cannabinoids
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Neurotransmitters in the CNS
THC; memory, cognition, pain |
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Barbiturates
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Sedative-Hypnotic & Anti-Anxiety Drugs
Bind GABAA, enhance axn independent of GABA; hypnosis; Low safety margin; life threatening withdrawal; schedule II of III; synergy w/ etoh; Cyp450 inducer SE: CNS depression, mood distortion, ↓respiratory drive, ↓BP, ↓REM sleep CI: porphyria; Tx of OD: diuresis/alkalinization of urine, don’t give stimulant |
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Phenobarbital
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Sedative-Hypnotic & Anti-Anxiety Drugs
Barbiturates anticonvulsant |
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Thiopental
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Sedative-Hypnotic & Anti-Anxiety Drugs
Barbiturates ultra short acting; anesthesia induction |
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Benzodiazepines
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Sedative-Hypnotic & Anti-Anxiety Drugs
Bind GABAA complex, enhance axn only when GABA is present → ceiling effect, relatively safe; liver met (no Cyp); synergy w/ etoh; schedule IV Eff: anti-anxiety, sedation, muscle relax, anticonvulsant SE: CNS depression, drowsiness, memory loss; esp. in elderly Tolerance: when used chronically, discontinuation → insomnia, anxiety, seizures CI: pregnancy, children, sleep apnea Tx: anxiety except OCD, PTSD, agoraphobia, children |
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Diazepam (Valium)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines long T1/2; tx: status epilepticus, etoh/barb w/drawl, DT’s, muscle spasm |
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Chlordiazepoxide (Librium)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines long T1/2; tx: etoh w/drawl, DT’s |
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Flurazepam (Dalmane)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines long T1/2; hypnotic |
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Lorazepam (Ativan)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines int T1/2; tx: status epilepticus |
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Alprazolam (Xanax)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines short T1/2; anxiety + depression |
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Midazolam (Versed)
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Sedative-Hypnotic & Anti-Anxiety Drugs
Benzodiazepines very short T1/2; sedation, calming, amnesia in surgery |
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Temazepam (Restoril), Triazolam (Halcion)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Benzodiazepines hypnotic |
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Clonazepam (Klonopin)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Benzodiazepines tx: seizures |
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Flumazenil
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Benzo Antagonist competitive antagonist; tx: reverse CNS depression in anesthesia or OD SE: trigger w/drawl & seizures in dependent pts |
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Others (Anti-anxiety & Sedatives)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) Bind BZ receptor with some GABA enhancing effects; strong sedatives, minor effect on REM sleep; liver met & kidney excretion; low dependence SE: drowsiness, blackouts - sleepwalking |
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Zolpidem (Ambien)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) BZ1 receptor, 2 hour T1/2 |
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Zaleplon (Sonata)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) BZ1 receptor, 1 hour T1/2 |
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Eszopiclone (Lunesta)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) 6 hour T1/2; tx: long term insomnia |
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Ramelteon (Rozerem)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) melatonin agonist; sleep aid; CI: sever liver disease |
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Buspirone (BuSpar)
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) 5HT1A partial agonist; tx: anxiety w/out causing sedation; 2 weeks for effect; very low addiction potential; little to no sedation; SE: restlessness, Intraxn: ↑BP with MAOI’s |
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Kava
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Sedative-Hypnotic & Anti-Anxiety Drugs.
Others (Anti-anxiety & Sedatives) herbal anti-anxiety; not FDA approved; SE: liver toxicity; CI: pregnancy |
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Alcoholism & Withdrawal
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Alcoholism & Withdrawal
Alcohol → (+) on GABA, (-) on NMDA; Chronic → ↓GABA, ↑ NMDA receptors, induces Cyp2E1 (↑ Tylenol met & toxicity); vasodilator, diuretic, cardiotoxic; alcohol (alcohol dehydrogenase) → acetaldehyde (aldehyde dehydrogenase) → acetate; Toxicity: emesis, coma, ↓respiration, death, also electrolyte disturbances, cutaneous vaso-D Withdrawal: can last up to 5 days; anxiety, nightmares, tachy, hallucinations, DT’s, seizures, arrhythmias, ↑BP |
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Diazepam, Chlordiazepoxide
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Alcoholism & Withdrawal
long acting benzo’s; tx: taper withdrawal |
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Haloperidol
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Alcoholism & Withdrawal
anti-psychotic, D2 block; tx: hallucinations, aggression |
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Naltrexone
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Alcoholism & Withdrawal
opioid rec antagonist; ↓reward & craving; SE: nausea, liver damage |
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Acamprosate
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Alcoholism & Withdrawal
GABA analogue; restores balance of GABA-Glutamate (NMDA); kidney excretion, no liver toxicity |
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Disulfiram (Antabuse)
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Alcoholism & Withdrawal
blocks aldehyde dehydrogenase→ ↑flushing, headache, nausea, confusion; long duration (3-4 days); dangerous, NR |
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Methanol (alcohol dehydrogenase)
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Alcoholism & Withdrawal
Methanol & Ethylene Glycol Poisoning Methanol to formaldehyde →formic acid - this is bad - visual disturbances, bradycardia, coma |
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Ethylene glycol
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Alcoholism & Withdrawal
Methanol & Ethylene Glycol Poisoning antifreeze (alc dh) → aldehydes & oxalates – also negative - metabolic acidosis |
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Ethanol
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Alcoholism & Withdrawal
Methanol & Ethylene Glycol Poisoning better substrate for alcohol dehydrogenase, ↓ formation of toxic metabolites |
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Fomepizole
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Alcoholism & Withdrawal
Methanol & Ethylene Glycol Poisoning alcohol dehydrogenase inhibitor, ↓ formation of toxic metabolites |
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Antidepressants
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All but one act on 5HT & NE
Antidepressant effect takes 2-3 weeks to develop |
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Tricyclic Antidepressants
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Antidepressants
Inh reuptake of 5HT & NE; also block M, α, and H receptors; no euphoria; liver met SE: sedation (H block), memory loss (Ach block), analgesia (↑NE), cardiac irritability (torsades), α1 block – postural hypotension, reflex tachy, dry mouth; weight gain, ↓seizure threshold, SIADH, sexual dysfunction, suicidal tendencies Drug Intraxn: MAOI’s → serotonin syndrome – hyperpyrexia, seizures, coma; wait 2-3 weeks after MAOI; SSRI’s - ↑TCA levels, toxicity; Amphetamine – hypertension; Cocaine – arrhythmias Tx: depression, panic attacks, chronic pain, fibromyalgia, neuropathic pain, enuresis |
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Amitriptyline, Imipramine
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Antidepressants
Tricyclic Antidepressants tertiary amine; more sedating; → active metabolite (Nor, Des) |
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Nortriptyline, Desipramine
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Antidepressants
Tricyclic Antidepressants secondary amine; less sedating; active form |
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MAO Inhibitors
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Antidepressants
MAO-A breaks down 5HT & NE and tyramine; MAO-B – breaks down dopamine; MAOI’s irreversibly inhibit MAO-A & B; long T1/2; liver met; Tx: depression SE: orthostatic hypotension, weight gain, α block-dry mouth, headache, blurred vision; sexual dysfunction Drug Intraxn: Tyramine in food (red wine, beer, cheese) – hypertensive crisis; Sudafed/ Amphetamine – hypertension; SSRI’s/ TCA’s/Meperidine – serotonin syndrome - Phenelzine (Nardil) - MAOI SSRI’s Inh 5HT reuptake; take 2-3 weeks for effect; mild SE’s SE: GI upset, weight loss, CNS stimulation – anxiety, insomnia; sexual dysfunction Drug Intraxn: MAOI’s/St John’s Wart – serotonin syndrome; TCA’s - ↑TCA levels, toxicity; Opioids (w/ fluoxetine) - ↓ opioid effect |
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Fluoxetine (Prozac)
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Antidepressants
MAO Inhibitors very long T1/2, 5 weeks to clear; inh Cyp2D6 |
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Paroxetine (Paxil)
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Antidepressants
MAO Inhibitors inh Cyp2D6; tx: OCD, agoraphobia, elderly; SE: sedation, anorexia |
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Sertraline (Zoloft)
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Antidepressants
MAO Inhibitors more selective, shorter T1/2 |
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Citalopram (Celexa), Escitalopram (Lexapro)
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Antidepressants
MAO Inhibitors faster onset (1-2 weeks), fewer intraxns |
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Venlafaxine (Effexor)
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Antidepressants
Inh 5HT & NE reuptake; tx: depression more SE’s, ↑BP |
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Duloxetine (Cymbalta)
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Antidepressants - Others
Inh 5HT & NE reuptake; tx: depression, neuropathic pain; hepatotoxic |
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Bupropion (Wellbutrin)
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Antidepressants - Others
Inh Dopamine reuptake; tx: depression, ADHD, smoking cessation; less sexual dysfunction; CI: pts w/ seizures or head trauma |
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Mirtazapine (Remeron)
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Antidepressants - Others
blocks α2→↑5HT & NE but blocks 5HT2A, 3 receptors→ fewer SSRI SE’s (less sexual dysfunction); tx: depression SE: sedation |
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Trazodone
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Antidepressants - Others
partial agonist at 5HT1A & blocks 5HT2; tx: sleep aid, pain; SE: sedation, priapism |
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St John’s Wart
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Antidepressants - Others
may block 5HT & NE reuptake; SE: sun sensitivity, P450 inducer; Intraxn: MAOI’s, SSRI’s, TCA’s, l-dopa, ↑general anesthetic effect |
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Schizophrenia
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hallucinations, lack of affect, apathy, delusions; ↑dopaminergic activity
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Dopaminergic system
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Anti-Psychotic Drugs & Mood Stabilizers
Nigrostriatal - SN to caudate/putamen (part of striatum); posture & movement; ↓ in activity → extrapyramidal symptoms (Parkinson’s) Mesolimbic-Mesocortical – ventral tegmental area (midbrain) to limbic-nucleus accumbens (striatum)/frontal cortex; reward, emotions, cognition; ↑ activity → psychosis Pituitary – Arcuate nuc (hypothalamus) to ant pituitary; inh prolactin secretion D2 block for tx of “positive” symptoms - delusions D4 & 5HT2A block for tx of “negative” symptoms – apathy |
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Extrapyramidal symptoms (EP’s)
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Anti-Psychotic Drugs & Mood Stabilizers
akathisia, dystonia, tremor, tardive dyskinesia: tx by bringing dopamine and Ach activity into balance; so drugs with more anti-Ach have ↓EP symptoms |
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Phenothiazines
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Anti-Psychotic Drugs & Mood Stabilizers
Block D2, α, H, and anti-Ach effect Effect: ↓ fear, ↓hallucinations, ↓anxiety, antiemetic SE: weight gain, ↑prolactin, dry mouth, orthostatic hypotension, sexual dysfunction, sedation, ↓seizure threshold, neuroleptic malignant syndrome, EP’s |
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Chlorpromazine
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Anti-Psychotic Drugs & Mood Stabilizers
tx: schizo, nausea, mania, hallucinations; SE: mild jaundice |
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Thioridazine
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Anti-Psychotic Drugs & Mood Stabilizers
more anti-Ach → ↓EP’s, ↑sedation, hypotension |
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Prochlorperazine (Compazine)
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Anti-Psychotic Drugs & Mood Stabilizers
antiemetic |
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Haloperidol (Haldol)
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Anti-Psychotic Drugs & Mood Stabilizers
more selective block of D2 w/ some effect on α and 5HT2; tx: acute psychosis; SE: many EP symptoms |
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New Generation/Atypical Antipsychotics
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Anti-Psychotic Drugs & Mood Stabilizers
SE: weight gain, sedation |
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Clozapine
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics – D2, D4, & 5HT2A block; blocks α1, H, and anti-Ach effect; ↓ EP symptoms, few prolactin effects; SE: agranulocytosis – frequent blood tests required |
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Quetiapine
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics like Clozapine but no agranulocytosis; ↓EP’s, ↓prolactin effects |
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Olanzapine
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics D2, D4, & 5HT2A block; anti-Ach effect; ↓ EP symptoms; Tx: bipolar, negative symptoms; SE: Type II Diabetes/hyperglycemia |
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Risperidone
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics 5HT2A, D2, & α block; enhances DA in basal ganglia ↓ EP symptoms; SE: postural hypotension, long QT, ↑prolactin |
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Ziprasidone
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics like Risperidone; some antidepressant effect |
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Aripiprazole (Abilify)
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Anti-Psychotic Drugs & Mood Stabilizers
New Generation/Atypical Antipsychotics blocks 5HT2A; partial agonist at D2 & 5HT1A; “dopamine stabilizer”; ↓EP’s, ↓prolactin effects; SE: orthostatic hypotension, hyperglycemia, ↓esophageal motility, sedation, seizures |
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Mood Stabilizers
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Anti-Psychotic Drugs & Mood Stabilizers
Tx: bipolar disorder |
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Lithium
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Anti-Psychotic Drugs & Mood Stabilizers
Mood Stabilizers kidney excretion, competes w/ Na for resorption; Thiazides, NSAID’s, & ↓Na→↑ [Li]; SE: nausea, headache, tremor, ↓thyroid function, edema, weight gain, diabetes insipidus (tx w/ amiloride); narrow therapeutic range; Toxicity: nausea, tremor, fasciculations →confusion, ataxia, seizures, arrhythmias, coma |
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Valproic Acid, Divalproex
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Anti-Psychotic Drugs & Mood Stabilizers
Mood Stabilizers anticonvulsant and mood stabilizer; rapid onset; SE: GI upset, weight gain, liver damage |
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Carbamazepine
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Anti-Psychotic Drugs & Mood Stabilizers
Mood Stabilizers anticonvulsant and mood stabilizer; tx: neuropathic pain; CI: pregnancy |
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Topiramate
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Anti-Psychotic Drugs & Mood Stabilizers
Mood Stabilizers anticonvulsant; tx: neuropathic pain |
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Parkinson’s disease
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Parkinson’s and Alzheimer’s Drugs
Nigrostriatal dopaminergic neurons - SN to caudate/putamen (part of striatum); degeneration → ↓DA (& relative ↑Ach activity) → Parkinson’s DA metabolism – tyrosine → l-dopa (dopa decarboxylase) → dopamine (MAO-B & COMT) → HVA; DA doesn’t cross BBB, l-dopa does cross BBB |
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L-Dopa (Levodopa)
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Parkinson’s Disease Drugs
symptomatic relief only; greatly metabolized in GI and periphery → nausea |
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Carbidopa/Levodopa (Sinemet)
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Parkinson’s Disease Drugs
carbidopa: inh dopa decarboxylase; carbidopa does not cross BBB; ↑ l-dopa entry into brain→↓ dose required; ↓peripheral effects; ↓effectiveness w/ time (3-4 years) due to continued loss of DA neurons; SE: nausea, postural hypotension, psychosis, insomnia, dyskinesia, “on-off”; Intraxn: MAOI’s → hypertensive crisis; CI: psychosis, malignant melanoma |
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Selegiline
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Parkinson’s Disease Drugs
inh MAO-B; ↓ROS, may slow disease progression; used w/ l-dopa/carbidopa |
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Bromocriptine
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Parkinson’s Disease Drugs
direct DA receptor agonist→ effectiveness does not ↓ with time; SE: anorexia, nausea, erythromelalgia – red, tender, swollen feet; postural hypotension, arrhythmias, dyskinesia, delusions, |
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Pramipexole, Ropinirole
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Parkinson’s Disease Drugs
DA agonist; well tolerated, initial tx; ↓ “on-off”; SE: sudden sleep |
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Amantadine
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Parkinson’s Disease Drugs
antiviral; may ↑ DA release; SE: psychosis, seizures, spotting of skin |
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Benztropine (Cogentin)
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Parkinson’s Disease Drugs
anti-Ach; restores DA-Ach balance; ↓ tremor, ↓ rigidity; little effect on bradykinesia |
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COMT Inhibitors
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Parkinson’s Disease Drugs
Tolcapone, Entacapone – adjunct to levo/carbi |
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Alzheimer’s
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Confusion, memory loss, personality changes → anxiety, difficulty recognizing family/friends → loss of speech, appetite, bladder control
Degeneration of cholinergic neurons – nuc basalis of Meynert to cerebral cortex & hippocampus; ↓Ach levels; eventual ↓ in NE & 5HT |
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Memantine
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Alzheimer’s Drugs
NMDA antagonist – prevents glutamate neurotoxicity→ may slow disease progression; SE: agitation, incontinence, insomnia; Intraxn - enhances l-dopa adverse effects |
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Cholinesterase Inhibitors
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Alzheimer’s Drugs
Prolong Ach effect; improve symptoms until disease progresses |
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Donepezil (& Tacrine, Rivastigmine, Galantamine)
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Alzheimer’s Drugs
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Baclofen
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Centrally Acting Muscle Relaxants (Spasmolytics)
GABAB agonist→ pre-syn inhibition of excitatory NT release in brain/spinal cord; intrathecal; ↓spasticity, ↓pain; tx: chronic spasticity; SE: muscle weakness |
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Diazepam
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Centrally Acting Muscle Relaxants (Spasmolytics)
enhances GABAA in spinal cord; relaxes muscle/mind; tx: local muscle trauma SE: sedation |
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Cyclobenzaprine (Flexeril)
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Centrally Acting Muscle Relaxants (Spasmolytics)
CNS Depressants CNS depressant; anti-Ach activity; TCA like; tx: acute spasm; SE: sedation, confusion, hallucinations; drug of abuse |
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Carisoprodol (Soma)
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Centrally Acting Muscle Relaxants (Spasmolytics)
CNS Depressants CNS depressant; metabolized to meprobamate (barb. like); drug of abuse (soma-coma); tx: spasticity, pain; SE: sedation |
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Tizanidine
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Centrally Acting Muscle Relaxants (Spasmolytics)
Others α-2 agonist; tx: chronic spasticity, acute spasm; SE: sedation, hypotension |
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Dantrolene
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Centrally Acting Muscle Relaxants (Spasmolytics)
Others ↓Ca release in muscle (sarc reticulum); tx: malignant hypothermia, neuroleptic malignant syndrome (antipsychotics) |
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Botulinum Toxin (Botox)
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Centrally Acting Muscle Relaxants (Spasmolytics)
Others blocks Ach release; tx: control local spasm, remove wrinkles |
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CNS Stimulants
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↑DA (& NE) levels
Effects – Low dose: ↑BP, ↑alertness, ↓appetite, euphoria Med dose: tremor, restlessness, ↑respiration High dose: behavioral repetition, psychosis Physical dependence, abuse potential |
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Amphetamine (Adderall)
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CNS Stimulants
tx: ADHD, narcolepsy |
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Methylphenidate (Ritalin, Concerta)
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CNS Stimulants
tx: ADHD, narcolepsy |
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Atomoxetine (Strattera)
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CNS Stimulants
SNRI, (-)NE reuptake; tx: ADHD |
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Caffeine
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CNS Stimulants
blocks adenosine receptors, (-)PDE→ ↑cAMP; Eff: ↑alertness, ↑ gastric acid, diuresis vaso-C cerebral BV’s→ headache relief; High dose: tachy, hypertension, insomnia |
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Depression CNS Stimulants
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5HT
NE (DA) |
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Anxiety CNS Stimulants
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GABA
5HT |
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Seizures CNS Stimulants
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NMDA
GABA |
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Memory/Learning CNS Stimulants
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Ach
NMDA |
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Pain CNS Stimulants
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NE
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Schizo CNS Stimulants
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DA
Mesocortical |
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Partial Agonists – 5HT1A CNS Stimulants
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Buspirone
Aripiprazole & D2 (& blocks 5HT2) |
