PHARM FINAL DRUGS Flashcards
Chlorpromazine (Throrazine)
Phenothiazine, 1st generation antipsychotic (neuroleptic)
low potency, increased cardiovascular/sedation due to alpha, anticholinergic and histamine blocking
Fluphenazine (Prolixin, Prolixin Decanoate [IM])
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
*Available in long-acting depo forms (decanoate and enanthate)
Prochlorperazine (Compazine)
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
**Used as antiemetic
Trifluoperazine (Stelazine, Suprazine)
Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
Haloperidol (Haldol, Haldol Decanoate [IM])
Butyrophenone, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
Clozapine (Clozaril)
Atypical antipsychotic
Blocks mesolimbic dopamine receptors (D4), also blocks 5HT receptors, strong anticholinergic
Little EPS.
**Agranulocytopenia, and agranulocytosis,
Seizures, weight gain, hyperglycemia, T2D, myocarditis
TX: suicidal behavior
Olanzapine (Zyprexa)
Atypical antipsychotic Similar to clozapine, less bone marrow tox. **Weight gain, hyperglycemia >EPS than clozapine TX: schizo and mania
Risperidone (Risperdal)
Atypical antipsychotic Block D2/4 and 5TH receptors >EPS than clozapine and olanzapine **Weight gain and hyperglycemia *Most widely used, available in depo
Aripiprazole (Abilify)
Atypical antipsychotic
*MOA: partial agonist/antagonist at D2 and 5HT-1a receptors
less ESP, less metabolic issues, but less efficacious that clozapine/olanzapine/respiradone
Quetiapine (Seroquel)
Atypical antipsychotic
MOA similar to clozapine BUT less efficacious
Low tendency of EPS
**NO agranulocytosis, high cost
Ziprasidone (Geodon)
Atypical antipsychotic
Same as quetiapine:
MOA similar to clozapine BUT less efficacious
Low tendency of EPS
**NO agranulocytosis, high cost
**fewer metabolic complications (weight gain/hyperglycemia)
Antipsychotic 1st generation (neuroleptics) drug effects
only for positive symptoms
Sedation early in therapy. Lowers seizure threshold. Antiemetic - especially prochlorperazine. Poikilothermia. Anticholinergic** (dry mouth, loss of visual accommodation), constipation, urine retention). Antihistiminic action - sedation. Cardiovascular effects** (Orthostatic HypoTN, tachycardia, EKG changes, sudden cardiac death - Torsades). Sexual dysfunction (alpha blocking). Increased prolactin secretion (due to decreased dopamine) gynecomastia, lactation, menstrual problems. Weight gain, increased appetite, edema, and effect on insulin/glucose metabolism. Teratogenic
Antipsychotic 1st gen neuroleptics Toxicities
idiosyncratic/allergic - blood dyscrasias, obstructive jaundice, rash, phototoxicity, cardiotoxicity, increased mortality with comorbid dementia.
EPS - acute dystonia (days) TX: benztropine, Trihexiphenydyl
akathisia (days-weeks) TX: anticholinergic, propranolol, benzos
parkinsonism (days-months) TX: Anticholinergics
Tardive dyskinesia (Months-years) TX: none, may need to resume antipsychotic
NMS (days-weeks) TX: Dantrolene or bromocryptine (inhibit release of Ca from sarcoplasmic reticulum)
Imipramine (Tofranil, Janimine)
TCA - Prototype
See TCA effects/tox
Amitriptyline (Elavil)
TCA
**More sedation and anticholinergic activity than imipramine
Fluoxetine (Prozac)
SSRI
MOA: inhibitor of 5HT reuptake
Use: antidepressant, OCD, generalized anxiety, and premenstrual dyphoric disorder, bulimia, anorexia, other eating disorders.
**Less sedation, anticholinergic, and cardiovascular effects than typical TCAs
SEs: headache, anxiety, tremor, agitation, nausea, sexual dysfunction. Potential for drug interaction with liver metabolism +active metabolites
Fluvoxamine (Luvox)
SSRI
MOA same as fluoxetine
TX: OCD
Sertraline (Zoloft)
SSRI
MOA same as fluoxetine
Slow elimination
**Less sedation, anticholinergic, and cardiovascular effects than typical TCAs
SEs: headache, anxiety, tremor, agitation, nausea, sexual dysfunction. LESS potential for drug interaction with liver metabolism +active metabolites
Paroxetine (Paxil)
SSRI
MOA: same as fluoxetine
Less sedation, anticholinergic, and cardiovascular effects than typical TCAs
SEs: headache, anxiety, tremor, agitation, nausea, sexual dysfunction.Weight gain. Potential for drug interaction with liver metabolism +active metabolites
**Rapidly metabolized
Citalopram (Celexa)
SSRI
Similar to sertraline
**Fewer drug interactions
Escitalopram (Lexapro)
SSRI
Similar to sertraline
**Fewer drug interactions
Venlafaxine (Effexor)/desvenlafaxine (Pristiq)
SNRI
MOA: inhibits the reuptake of serotonin, norepinephrine, and dopamine.
Fewer cardiovascular effects, but still some hypertension and tachycardia in some populations. Mild stimulant effect.
SEs: nausea, nervousness, anxiety, sweating.
TX: depression and generalized anxiety disorder. May be useful for treatment of ADD in children
Duloxetine (Cymbalta)
SNRI
resembles venlafaxine
TX: neuropathic pain!
Trazodone (Desyrel)
Second gen antidepressant
MOA: inhibits reuptake of 5HT and block 5-HT2 receptors
**Less cardiovascular/anticholinergic effects than TCAs, but can cause sexual dysfunction
Very sedating, may be used as a night time med
Nefazodone (Serzone)
Second gen antidepressant
Similar to trazodone
Bupropion (Wellbutrin)
Second gen antidepressant
MOA: selectively blocks reuptake of dopamine
Mild stimulant activity, MORE likely the produce seizures
TX: nicotine, amphetamine, and cocaine dependence
Mirtazepine (Remeron)
Second gen antidepressant
MOA: block presynaptic alpha-2 adrenergic receptors - enhances synaptic release of NE and 5HT, blocks some subtypes of 5HT receptors
SEs: similar to TCAs
TX: may be useful in depressed patients with high levels of anxiety
Atomoxetine (Strattera)
Selective Norepinephrine Reuptake Inhibitor
TX: ADHD in children and adults
SEs: supression of appetite, decreased weight gain, HTN, Tachycardia, sexual dysfunction
Phenelzine (Nardil)
MAOI
Tranylcypromine (Parnate)
MAOI
Selegiline (Emsam)
MAOI
MOA: MOA-B inhibitor (irreversibly inactivates) - increases dopamine levels
*Available as patch for depression
**Used in treatment of parkinson’s
Lithium Carbonate (Eskalith, others)
Mood Stabilizer
MOA: 3 theories: ionic - may alter the neuronal distribution/effect of Na, K, or Ca, in the CNS, amine theory - later release/reuptake of neurotransmitter amines, phospholipid - alter metabolism of phospholipids that are involved in the phosphoinositide signaling pathway
*Currently the most effective treatment for manic-depressive disorders
Effects: controls mood swings
*Caution in patients with impaired renal function
NSAIDs, diuretics, etc, can alter renal excretion of lithium
*Must monitor serum lithium levels. Therapeutic range (0.8-1.4) toxicity >2.0
Acute Tox: n/v/d, fatigue, weakness, tremor, ataxia, blurred vision, tinnitus, slurred speech, dizziness, confusion, seizure, stupor, coma, arrhythmias, hypotension, circulatory collapse. **May appear to be drunk! Other: hypothyroid, polydipsia, polyuria, kidney damage NDI
TX of toxicity: supportive, diuresis, hemodialysis
Valproic Acid analog (Depakene, Depakote)
Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders
Carbamazepine (Tegretol)
Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders
Clonazepam (Klonopin)
Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders
TCA effects
Sedation - seen in early therapy. (Greatest in the TCAs > second gen drugs) Slow onset of action. CNS stimulation (some drugs) - tremor, restlessness, insomnia, irritability, seizures. Decreased seizure threshold.
Anticholinergic effects (dry mouth, constipation, urine retension, loss of visual accommodation) More sever than antipsychotic drugs (amitriptyline is the worse, SSRIs least)
CV side effects - postural hypoTN, tachycardia, flattening/inversion of the T wave, arrhythmias
TCA toxicities
Caution in patients with liver disease.
Anticholinergics
CNS - sedation, temor, agitation, anxiety, irritability, manic phase, parkinsonism (rare), seizure
Cardiovascular - hypotension, tachycardia, arrhythmias
Weights gain with TCAs
Impotence, teratogenic, blood dyscrasias
Acute poisoning - TX: sodium bicarbonate (reduces cardiotoxic effects)
Drug interactions - MAOIs can cause “serotonin syndrome” = tremors, HTN, hyperpyrexia, seizures
MAO-A
Preferentially metabolized NE and 5HT
MAO-B
Preferentially metabolizes dopamine
MAOIs effects/toxicity
CNS - normalizes sleep patterns, stimulation in some patients (tremors, insomnia, hallucinations) may switch to manic phase
TOX: orthostatic hypotension, HTN in overdose, GI - nausea, constipation; heachache, dizziness, vertigo, liver damage, allergies
**Interactions with foods and other drugs (TYRAMINE)
Tyramine (cheese toxicity) - stimulates the release of catecholamines, can lead to severe HTN, fever, and seizure
pheochromocytoma, sympathomimemtics (amphetamines, cocaine, dopamine), TCAs - fever, convulsions, death)
