Showing posts with label Psychopharmacological Agents. Show all posts
Showing posts with label Psychopharmacological Agents. Show all posts

Lithium Carbonate

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Name: Lithium Carbonate

Class: Psychopharmacological Agents (Mood Stabilizer)

Mechanism: Unknown, but may involve electrolyte/ion transport, enhanced reuptake of tryptophan ® ­ brain 5HT levels, inhib. of phosphatidyl inositol 2nd messenger system, ¯ DA & NE turnover, or ­ synth. of ACh.

Absorption:

Dist.:

Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Low TI (plasma levels must be monitored). Edema, sedation, fine tremor (treat w/propranolol), polyuria, thirst, gastric upset, mild diarrhea. Serious = coarse tremor, vomiting, profuse diarrhea, ataxia, cardiac arrhythmias, seizures, coma, death. ¯ thyroid fxn, but usu. asympt. Diuretics ® Na+ depletion ® ­ Li+ conc.

Utility: Prophylaxis for bipolar illness. Acute severe mania is more quickly controlled w/neuroleptics. Combination therapy often required.

Special Features:

 

Sertraline (Zoloft)

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Name: Sertraline (Zoloft)

Class: Psychopharmacological Agents (Antidepressant) (SSRI)

Mechanism: Blocks reuptake of serotonin.

Absorption:

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Toxicity/S.E.s: Anxiety, insomnia, restlessness, GI distress.

Utility: Treat depression.

Special Features:

 

Fluoxetine (Prozac)

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Name: Fluoxetine (Prozac)

Class: Psychopharmacological Agents (Antidepressant) (SSRI)

Mechanism: Blocks reuptake of serotonin.

Absorption:

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Excretion, t½:

Toxicity/S.E.s: Anxiety, insomnia, restlessness, GI distress.

Utility: Treat depression.

Special Features:

 

Tranylcypromine (Parnate)

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Name: Tranylcypromine (Parnate)

Class: Psychopharmacological Agents (Antidepressant) (MAOI) (Non-Hydrazine Deriv.)

Mechanism: Inhib. of MAO ® central build-up of NE, 5HT, DA.

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Toxicity/S.E.s: Headache, drowsiness, dry mouth, weight gain, postural hypotension (central a2), sexual disturbances, liver damage, hyperpyrexia. Interactions w/TCAs, dextromethorphan, mepiridine, and tyramine can be fatal.

Utility: Treat depression.

Special Features: Usu. prescribed as alt. only when other drugs are ineffective.

 

Phenelzine (Nardil)

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Name: Phenelzine (Nardil)

Class: Psychopharmacological Agents (Antidepressant) (MAOI) (Hydrazine Deriv.)

Mechanism: Inhib. of MAO ® central build-up of NE, 5HT, DA.

Absorption:

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Toxicity/S.E.s: Headache, drowsiness, dry mouth, weight gain, postural hypotension (central a2), sexual disturbances, liver damage, hyperpyrexia. Interactions w/TCAs, dextromethorphan, meperidine, and tyramine can be fatal.

Utility: Treat depression.

Special Features: Usu. prescribed as alt. only when other drugs are ineffective.

 

Amitryptiline (Elavil)

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Name: Amitryptiline (Elavil)

Class: Psychopharmacological Agents (Tricyclic Antidepressant)

Mechanism: Blocks NE and 5HT uptake. Also prominent muscarinic blockade. Possible mechs include down-reg. of brain a2 and 5HT2 receptors or decreased number of b brain receptors.

Absorption: Dist.: Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Prominent sedation, postural hypotension, excess sweating, marked ¯ in REM sleep. Anticholinergic effects. Block antihypertensive effects of guanethidine. Enhance effects of some sympathomimetics. Can be extremely toxic when combined w/MAO inhibs (but can also be done safely). Potentiates effects of alcohol and other CNS depressants. Overdoses ® coma, seizures, hypotension, depressed resp., arrhythmias.

Utility: Treat endogenous depression, enuresis, chronic pain, panic rxns, phobic anxiety.

Special Features: TCAs preferred over MAOIs for initial treatment of endogenous depression. Severely depressed patients should never be given more than a 1 week supply of a TCA (danger of overdose).

 

Imipramine (Tofranil)

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Name: Imipramine (Tofranil)

Class: Psychopharmacological Agents (Tricyclic Antidepressant)

Mechanism: Blocks NE and 5HT uptake. Also prominent muscarinic blockade. Possible mechs include down-reg. of brain a2 and 5HT2 receptors or decreased number of b brain receptors.

Absorption: Dist.: Metabolism.:

Excretion, t½:

Toxicity/S.E.s: Sedation, postural hypotension, excess sweating, marked decrease in REM sleep. Block antihypertensive effects of guanethidine. Enhance effects of some sympathomimetics. Can be extremely toxic when combined w/MAO inhibs (but can also be done safely). Potentiates effects of alcohol and other CNS depressants. Overdoses ® coma, seizures, hypotension, depressed resp., arrhythmias.

Utility: Treat endogenous depression, enuresis, chronic pain, panic rxns, phobic anxiety.

Special Features: TCAs preferred over MAOIs for initial treatment of endogenous depression. Severely depressed patients should never be given more than a 1 week supply of a TCA (danger of overdose).

 

Clozapine (Clozaril)

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Name: Clozapine (Clozaril)

Class: Psychopharmacological Agents (Antipsychotic) (Dibenzodiazepine Deriv.)

Mechanism: Blocks 5HT2, H1, a receptors. High D1 affinity, relatively low D2 affinity. Also acts on muscarinic and histaminic receptors.

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Toxicity/S.E.s: Sedation, seizures, antimuscarinic, activity, agranulocytosis (bone marrow toxicity). Close monitoring required (i.e., blood tests every couple of weeks). Drug interactions—w/some BZDs may cause death.

Utility: Treat schizophrenia, esp. patients w/tardive dyskinesia.

Special Features: Little, if any, tendency for extrapyramidal disorders. May even reverse them. More effective than other antipsychotics in relieving neg. symptoms of schizophrenia.

 

Haloperidol (Haldol)

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Name: Haloperidol (Haldol)

Class: Psychopharmacological Agents (Antipsychotic) (Butyrophenone Derivative)

Mechanism: Blocks DA (esp. in limbic areas), muscarinic, a-adrenergic, H1 histaminic, & 5-HT2 receptors.

Absorption: Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: High incidence of extrapyramidal toxicity. Early onset extrapyramidal disorders—pseudo-Parkinsonism, akathisia, acute dystonias (dosage reduction or anticholinergics help). Late onset extrapyram. disorder—tardive dyskinesia (can be irreversible). Hyperprolactinemia, amenorrhea, infertility. Antimuscarinic effects. Orthostatic hypotension, impotence (a). Sedation (H1). Weight gain. Allergic agranulocytosis (esp. w/clozapine (1-2%)). Neuroleptic malignant synd.—hyperpyrexia, catatonia, excessive muscle rigidity, altered mental status, ANS instability; incidence 1%, mortality 15%. For NMS stop Rx, admin. dantrolene (muscle relaxant) & dopamine agonists (e.g., bromocriptine). Drug interactions—may potentiate actions of other CNS depressants.

Utility: Treat schizophrenia, Tourette’s syndrome, manic episodes, intractable hiccough, emesis. Preanesthetic.

Features: Drug holidays important to reduce tendency for tardive dyskinesia and test for continued need. Big problem w/non-compliance. Limit doses to min. side effects.

 

Chlorpromazine (Thorazine)

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Name: Chlorpromazine (Thorazine)

Class: Psychopharmacological Agents (Antipsychotic) (Aliphatic Phenothiazine Derivative)

Mechanism: Blocks DA (esp. in limbic areas, CTZ, GI), muscarinic, a-adrenergic, H1 histaminic, & 5-HT2 receptors.

Absorption: Oral, suppository (emesis) Dist.: Metabolism.: Excretion, t½:

Toxicity/S.E.s: Early onset extrapyramidal disorders—pseudo-Parkinsonism, akathisia, acute dystonias (dosage reduction or anticholinergics help). Late onset extrapyram. disorder—tardive dyskinesia (can be irreversible). Hyperprolactinemia, amenorrhea, infertility. Antimuscarinic effects. Orthostatic hypotension, impotence (a). Sedation (H1). Weight gain. Allergic agranulocytosis. Neuroleptic malignant synd.—hyperpyrexia, catatonia, excessive muscle rigidity, altered mental status, ANS instability; incidence 1%, mortality 15%. For NMS stop Rx, admin. dantrolene (muscle relaxant) & dopamine agonists (e.g., bromocriptine). Drug interactions—may potentiate actions of other CNS depressants.

Utility: Treat schizophrenia, manic episodes, intractable hiccough. Treat emesis from drugs, radiation, uremia, pain, post-op, emotional, GI irritation, cancer chemotherapy. Preanesthetic.

Features: Drug holidays important to reduce tendency for tardive dyskinesia and test for continued need. Big problem w/non-compliance. Limit doses to min. side effects. No potential for abuse.