Antipsychotics/sedatives & Hypnotics/antidepressants/antiepileptics

Front 1

Low potency, Aliphatic Phenothiazine, Used to treat Schizophrenia, acute mania, Tourette's and as an antiemetic. Dopamine Receptor (D2) Antagonist. Also antagonize Histamine H1 receptors and alpha adrenergic receptors in the peripheral NS.

Back 1

Chlorpromazine

Hint 1

SE: Agranulocytosis, Sexual Dysfunction, Sedation, Anticholinergic crisis, Do not combine with CNS depressants.

Front 2

Low Potency, Piperidine Antipsychotic. Dopamine Receptor (D2) Antagonist. Also antagonize Histamine H1 receptors and alpha adrenergic receptors in the peripheral NS.

Back 2

Thioridazine.

Hint 2

Increases QT interval, can cause sudden death with overdose.

Front 3

High Potency, Peperazine (2 drugs here). Dopamine Receptor (D2) Antagonist. Also antagonize Histamine H1 receptors and alpha adrenergic receptors in the peripheral NS.

Back 3

Fluphenazine, Trifluperazine

Hint 3

Tardive Dyskinesia! Extrapyramidal syndromes.

Front 4

Butyrophenone, high oral potency, antipsychotic. Slow release form available. Dopamine Receptor (D2) Antagonist. Also antagonize Histamine H1 receptors and alpha adrenergic receptors in the peripheral NS.

Back 4

Haloperidol

Hint 4

Extrapyramidal syndromes. Tardive Dyskinesia.

Front 5

Atypical Antipsychotic, Causes much concern for the possibility of agranulocytosis. Does not elevate serum PROLACTIN levels. Antagonist at D2, D4 and 5HT2a Receptors (Serotonin Receptor Antagonist).

Back 5

Clozapine

Hint 5

Last resort. Weight gain, postural hypotension, sedation, impotence.

Front 6

Atypical Antipsychotic. Does not cause agranulocytosis. Antagonist at D2, D4 and 5HT2a Receptors (Serotonin Receptor Antagonist).

Back 6

Risperidone

Hint 6

Hyperprolactinemia. Sedation. Impotence.

Front 7

Atypical Antipsychotic. NO AGRANULOCYTOSIS OR HYPERPROLACTINEMIA! Less likely to cause EPS or TD. Lower incidence of sexual dysfunction. Antagonist at D2, D4 and 5HT2a Receptors (Serotonin Receptor Antagonist).

Back 7

Olanzapine.

Hint 7

Postural Hypotension, lowering of seizure threshold, SIGNIFICANT SEDATION, CONSTIPATION AND WEIGHT GAIN and increased lipids and an association with development of DM.

Front 8

Action of Benzodiazepine

Back 8

Allosterically increases the frequency of GABA stimulated chloride channel opening, causing hyperpolarization.

Front 9

Indication for Benzodiazepine

Back 9

Anxiety (Situational, GAD, Panic disorger, Social, OCD), Insomnia, Status Apilepticus, Pre-anesthetic for short procedures, Muscle Relaxation in CP, Physical Dependence or Withdrawal from EtOH or barbituates. Acute Mania or Bipolar Dz.

Front 10

Xanax, a benzodiazepine. Indicated for Anxiety.

Back 10

Alprazolam

Hint 10

SE: sedation, ataxia, confusion, anterograde amnesia, tolerance develops

Front 11

Sedative/hypnotics (2) that are indicated for physical dependence or withdrawal.

Back 11

Diazepam (Valium) or Chlordiazepoxide (Librium).

Hint 11

Diazepam rapidly redistributes to periphery. Can also be used for status epilepticus. undergoes N-dalkylation to Desmethyldiazepam. SE: sedation, ataxia, confusion, anterograde amnesia, tolerance develops

Front 12

Benzodiazepines that are indicated for Insomnia to INDUCE sleep.

Back 12

Lorazepam and Triazolam

Hint 12

Lorazepam can also be used for status epilepticus. (Ativan)

Front 13

Benzodiazepines that are used to MAINTAIN sleep for insomniacs.

Back 13

Temazepam (Restoril) and Flurazepam (Dalmane)

Hint 13

Flurazepam rapidly redistributes to the periphery.

Front 14

Benzodiazepine used for short medical and surgical procedures as a pre-anasthetic.

Back 14

Midazolam (Versed)

Hint 14

Short DoA, hypnotic, reduces anxiety, amnestic effects. Used parenterally.

Front 15

Benzodiazepine used for muscle relaxation.

Back 15

Diazepam (Valium)

Hint 15

also used for status epilepticus and physical dependence or withdrawal.

Front 16

Benzodiazepine used for Physical Dependence or Withdrawal (looking for 2 drugs here)

Back 16

Diazepam (Valium) or Chlordiazepoxide (Librium)

Hint 16

For EtOH or Barbituate addiction. Also BZ dependence.

Front 17

BZ decarboxylated in gastric juice to active metabolite N-desmethyldiazepam (it's active metabolite is nordiazepoxide)

Back 17

Clorazepate

Front 18

Adverse Effects of BZ

Back 18

Sedation, Drowsiness, Ataxia and Confusion (CNS Depression), Anterograde Amnesia, Enhances Respiratory Depression in COPD Patients.

Front 19

Tolerance and Dependence of BZ

Back 19

Use length is 3-4 wks tops. tolerance develops, including cross tolerance with alcohol. Abuse potential is low. Withdrawal includes very severe anxiety, possible seizures and insomnia.

Front 20

Drug interactions with BZ.

Back 20

ALCOHOL! Combination is often deadly.

Front 21

Very selective, non-BZ, Serotonin (5HT1a) receptor partial agonist. Used to treat chronic GAD. Very specific for anxiety. No sedation, hypnosis or physical dependence. Slow Onset.

Back 21

Buspirone (Buspar)

Hint 21

May cause nervousness, restlessness, dysphoria, tachycardia or GI distress.

Front 22

Non-BZ, with a rapid onset and short DOA used for the short-term treatment of insomnia. Increases Cl- conductance stimulated by GABA by binding only to GABAa receptor isoforms that contain the alpha 1 subunit. Minimal tolerance and dependence. Less amnesia and daytime sedation. (3 drugs here)

Back 22

Zolpiden (Ambien), Zaleplon (Sonata), Eszoplicone (Lunesta)

Hint 22

Also acts selectively at BZ1 receptors.

Front 23

BZ-receptor agonist used to TREAT BZ OVERDOSE or to speed recovery from BZ in anesthetic and diagnostic procedures.

Back 23

Flumazenil

Hint 23

Very short DOA, Can precipitate withdrawal symptoms.

Front 24

Adverse effects of SSRI's.

Back 24

5HT syndrome especially with MAOi's, HA, SEXUAL DYSFUNCTION, Excitation, Anxiety, Apathy, Weight change, Apathy

Front 25

SSRI, least specific, very lon half life due to active metabolite. Inhibits liver microsomal enzymes.

Back 25

Fluoxetine (Prozac)

Front 26

Other 2 SSRI's that aren't Fluoxetine (Prozac)

Back 26

Sertraline (Zoloft) and Paroxetine (Paxil).

Front 27

Atypical antidepressant that is efficacious for mild depression. Affects liver metabolic pathways of many drugs.

Back 27

Hypercium (St. John's Wort)

Front 28

Atypical antidepressant who's metabolite blocks DA receptors. Induces hyperprolactinemia and has EPS/TD side effects.

Back 28

Amoxapine

Front 29

Atypical Antidepressant that antagonizes the 5HT2 serotonin receptor and causes MODERATE sedation.

Back 29

Nefazadone (Serzone)

Hint 29

Priapism!

Front 30

Atypical Antidepressant that antagonizes the 5HT2 serotonin receptor and causes SEVERE sedation.

Back 30

Trazadone (Desyrel)

Hint 30

Priapism!

Front 31

Atypical Antidepressants (2 here) that block Serotonin and NE reuptake receptors.

Back 31

Venlafaxine (Effexor) and Duloxetine (Cymbalta)

Hint 31

Prescribe if there is no response from SSRI's. Can produce SEIZURES when Venlafaxine treatment is discontinued.

Front 32

Atypical AD who's mechanism is uncertain. Low SE profile. Less sexual dysfunction. Can cause stimulation and sedation. Lowers seizure threshold and is more likely than TCA to cause seizures.

Back 32

Bupropion (Wellbutrin)

Hint 32

Also marketed as sustained release aid in smoking cessation (Zyban)

Front 33

Atypical AD that blocks pre-junctional alpha 2 receptors, increasing NE and 5HT neurotransmission. Also blocks serotonin 5HT2 and 5HT3 receptors. Sedation and weight gain are some of the FEW ADVERSE EFFECTS.

Back 33

Miertazapine (Remeron)

Front 34

Tertiary TCA but relatively 5HT specific. Approved only for OCD!

Back 34

Clomipramine (Anafranil)

Hint 34

Lethal in overdose. High incidence of seizures.

Front 35

Mechanism of TCA

Back 35

Blocks the reuptake of catecholamines by specific transporters into prejunctional nerve endings. Tertiary amines tend to block NE and Serotonin transporters, while secondary amines are more specific for NE transporter.

Front 36

Adverse effects of TCA's

Back 36

Accounted for by their antagonist activity at alpha-adrenoreceptors, muscarinic cholinoceptors (Confusion, Delerium, Memory Dysfunction) and histamine H1 receptors (Sedation and Drowsiness). Mania, Lower Seizure Threshold, Tremor (managed by propanolol). Postural hypotension, Dry mouth, blurred vision, constipation, weight gain (H1 antagonism), SEXUAL DYSFUNCTION.

Hint 36

Amoxapine specifically causes EPS and TD. Rebound effects make withdrawal needing to be tapered. Suicide is a major risk for patients under 24 y/o. Muscarinic Cholinoceptor and alpha adrenoceptor antagonist activity can put the patient into a coma, and eventually cause death. Prolongs QT interval.

Front 37

Drug interactions of TCA

Back 37

CNS depressants (EtOH), MAOi precipitate serotonin syndrome.

Front 38

TCA's (drug examples)

Back 38

Imipramine, Amitriptyline, Nortriptyline, Amoxapine (blocks DA receptors, too), Clomipramine.

Front 39

MAOi Mechanism

Back 39

Irreversible suicide inhibitors of MAO-A and B. Used to treat patients that respond poorly to TCA and SSRI treatment and patients with atypical depression.

Front 40

MAOi Adverse effects and drug interactions

Back 40

Hypotension, HA, Dry Mouth, Sexual Dysfunction. Worry about slow acetylators. AVOID TYRAMINE, because it causes release of NE.

Hint 40

Avoid SSRI, TCA and opioids because they may precipitate serotonin syndrome.

Front 41

The only MOAi we are responsible for.

Back 41

Phenelzine (Nardil)

Hint 41

MAOi's are a 3rd line treatment of depression.

Front 42

Mood stabilizer use to treat acute mania or bipolar (manic depressive disease). 40-70% effective. Protects against suicide.

Back 42

Lithium

Hint 42

SE: N/V, Acne, polyuria, polydipsia, tremor, coma, Thyroid enlargement (benign), Risk of fetal malformations of the CV system suring the 1st trimester. Depletes Na+. NSAID's CI except ASA or Acetomenophin

Front 43

Need to know that these two anti-convulsant drugs are use to treat mania or bipolar disease, either alone or as adjuncts to lithium therapy.

Back 43

Carbamazepine (Tegretol) and Valproic Acid (Depakote)

Front 44

Pharmacologic properties of Lithium

Back 44

Low therapeutic index, and thus plasma levels must be monitored continuously. Directly competes with Na+ in kidney. Therapeutic efficacy and adverse effects are directly related to its level in the blood.

Front 45

Anti-epileptic used for partial and tonic-clonic seizures. At high doses metabolism becomes zero order. Has a very low Therapeutic Index. Can cause fetal malformations and severe rashes.

Back 45

Phenytoin and Fosphenytoin

Hint 45

Increases metabolism of oral contraceptives. Common SE: ataxia, gingival hyperplasia, hirsutism and mental confusion. Carbamazepine and phenobarbital increase metabolism of phentoin. Cimetidin decreases metabolism of phenytoin.

Front 46

Anti-Epileptic used for partial and tonic-clonic seizures. Can cause hyponatremia due to water retention. Want to supplement folic acid for women during pregnancy. Same MOA as Phenytoin.

Back 46

Carbamazepine

Front 47

MOA of Phenytoin and Carbamazepine

Back 47

blocks Na+ channels in their inactive state prolonging cell refractoriness

Front 48

Anti-Epileptic for absence and myoclonic seizures. Has a fairly rough and unique SE profile. MOA is unclear.

Back 48

Valproic Acid

Hint 48

SE: severe N/V, weight gain, hair loss, ataxia and a FINE TREMOR. Inhibits the metabolism of carbamazepine and phenytoin.

Front 49

Drug of choice for ABSENCE seizures. Reduces the low threshold T-type Ca2+ current that provides pacemaker activity in the thalamus.

Back 49

Ethosuximide

Front 50

Primary drug for the treatment of febrile seizures in infants and status epilepticus.

Back 50

Phenobarbital

Hint 50

Facilitates GABA mediated inhibition of neuronal activity.

Front 51

Drug of choice for immediate treatment of Status Epilepticus

Back 51

Diazepam and Lorazepam (IV)

Hint 51

Facilitate GABA mediated inhibition of neuronal activity. SE: sedation and paradoxical hyperactivity in children.

Front 52

Adjunct or monotherapy for partial seizures. Voltage and use-dependent Na+ channel blockade.

Back 52

Lamotrigene

Hint 52

SE: HA, diplopia, nausea, skin rash.