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36 Cards in this Set

  • Front
  • Back

Histamine is metabolized by the enzymes

Monoamine oxidase and diamine oxidase

Excess production of histamine can be detected by it's major metabolite

Imidazole acetic acid

H1 antagonist drugs

Diphenhydramine


Promethazine


Chlorpheniramine


Meclizine

Diphenhydramine

Widley used otc drug, prototype

Promethazine

Some alpha blockade and Local anesthetic action

Chlorpheniramine

CNS stimulation

Meclizine

Highly effective in motion sickness

Second generation drugs do not cross blood brain and therefore have

No Antimuscarinic activity


No sedation


No antimotion sickness

Second generation drugs examples

Cetrizine


Loratidine


Fexofenadine

Which drugs have longer half life

Second generation

Clinical use of h1 antagonists

Allergies


Motion sickness


Diphenhydramine is used for chemotherapy induced vomitting


Toxicity and interactions of h1 antagonists

Sedation -1st generation


Interactions


Azoles antifungal drugs - inhibit hepatic metabolism


H2 antagonist drugs

Cimetidine


Ranitidine


Nizatidine


Famotidine

H2 used in


PUD


GERD

H2 interaction

Cimetidine is a potent inhibitor of P450


Antiandrogen effects in high doses

Serotonin agonists site of action and uses

.

Sumatriptan

Sumatriptan- 5ht1d. CI in patients with angina, migraine

Busiprone

Busiprone- 5ht1a- anxiety

Which serotonin agonist can cause fatal arrhythmias?

Cisapride

Serotonin Antagonists site of action and clinical uses

.

Cyproheptadine and methysergide

5HT2


Treat carcinoid syndrome

Ketanserin

5HT2A


Treat hypertension because of vasodilation properties

Ondansetron, Tropisetron, Granisetron

5-HT3


Anti-emetic and useful in control of vomitting in chemo

Fluoxetine

Selective serotonin reuptake inhibitor


Anti depressant and other uses

What drugs antagonize platelet agregation?

Ketanserin


Ritanserin

Serotonin syndrome can be precipitated by the drugs

SSRIs


Second generation antidepressants


Odansetron


Sumatriptan

Serotonin syndrome symptoms

Hypertension


Hyperrefflexia


Tremor


Hyperthermia


Hyperactive bowel sounds


Diarrhea


Mydriasis


agitation


Coma; onset within hours


ADR of ketanserin

Alpha blockade


Alternative - Ritanserin

Uses of ergot alkaloids

.

Effect and use of Ergotamine

Causes marked and prolonged alpha receptor mediated vasoconstriction


Used in acute attacks of migraine

Effect and use of Ergovine

Produce powerful contraction in the uterus


Reduction of post partum bleeding(maleate form only)


Diagnosis of variant angina

Treatment of Hyperprolactinemia

Bromociptine and peroglide- have cardiovascular toxicity


And


Cabergoline

Toxicity of ergotamine can cause

Vascular effects- Prolonged vasoconstriction which can cause ischemia and gangrene


GIT effects- nausea vomitting diarrhea


Uterine effects- uterine contraction that rarely lead to abortion


Methsergide is used for

Inducing hallucinations

Contradictions of ergot alkaloids

Obstructive vascular disease


Symptomatic coronary disease


Collagen disease


Pregnancy

Therapy for erogtamine toxicity

Nitroprusside