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Flashcards in PHARM FINAL DRUGS Deck (40):
1

Chlorpromazine (Throrazine)

Phenothiazine, 1st generation antipsychotic (neuroleptic)
low potency, increased cardiovascular/sedation due to alpha, anticholinergic and histamine blocking

2

Fluphenazine (Prolixin, Prolixin Decanoate [IM])

Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
*Available in long-acting depo forms (decanoate and enanthate)

3

Prochlorperazine (Compazine)

Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS
**Used as antiemetic

4

Trifluoperazine (Stelazine, Suprazine)

Phenothiazine, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS

5

Haloperidol (Haldol, Haldol Decanoate [IM])

Butyrophenone, 1st gen antipsychotic (neuroleptic)
high potency - greater EPS

6

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

7

Olanzapine (Zyprexa)

Atypical antipsychotic
Similar to clozapine, less bone marrow tox.
**Weight gain, hyperglycemia
>EPS than clozapine
TX: schizo and mania

8

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

9

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

10

Quetiapine (Seroquel)

Atypical antipsychotic
MOA similar to clozapine BUT less efficacious
Low tendency of EPS
**NO agranulocytosis, high cost

11

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)

12

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

13

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)

14

Imipramine (Tofranil, Janimine)

TCA - Prototype
See TCA effects/tox

15

Amitriptyline (Elavil)

TCA
**More sedation and anticholinergic activity than imipramine

16

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

17

Fluvoxamine (Luvox)

SSRI
MOA same as fluoxetine
TX: OCD

18

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

19

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

20

Citalopram (Celexa)

SSRI
Similar to sertraline
**Fewer drug interactions

21

Escitalopram (Lexapro)

SSRI
Similar to sertraline
**Fewer drug interactions

22

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

23

Duloxetine (Cymbalta)

SNRI
resembles venlafaxine
TX: neuropathic pain!

24

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

25

Nefazodone (Serzone)

Second gen antidepressant
Similar to trazodone

26

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

27

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

28

Atomoxetine (Strattera)

Selective Norepinephrine Reuptake Inhibitor
TX: ADHD in children and adults
SEs: supression of appetite, decreased weight gain, HTN, Tachycardia, sexual dysfunction

29

Phenelzine (Nardil)

MAOI

30

Tranylcypromine (Parnate)

MAOI

31

Selegiline (Emsam)

MAOI
MOA: MOA-B inhibitor (irreversibly inactivates) - increases dopamine levels
*Available as patch for depression
**Used in treatment of parkinson's

32

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

33

Valproic Acid analog (Depakene, Depakote)

Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders

34

Carbamazepine (Tegretol)

Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders

35

Clonazepam (Klonopin)

Mood Stabilizer
anti-epileptic, useful in manic-depressive disorders

36

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

37

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

38

MAO-A

Preferentially metabolized NE and 5HT

39

MAO-B

Preferentially metabolizes dopamine

40

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)