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AntiHistamines & Migraine Drugs
IUSM
16
Pharmacology
Professional
11/25/2014

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Cards

Term
diphenhydramine
Definition
Class: antihistamine, H1 antagonist, 1st gen

Mechanism: antagonist at H1 receptors, some antimuscarinic activity

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp, sleep aid, prophylaxis and tx motion sickness, REDUCE PARKINSON'S SYMPTOMS

Adverse effects: "drowsiness, sedation"; dizziness, lassitude, fatigue, nervousness, insomnia, tremor, loss of appetite, nausea, vomit, hypersensitivity rxn, dry mouth, blurred vision, urinary retention

Pharmacokinetics:
Absorption - well in GI
Distribution - hihgly lipid soluble, easy to CNS
Metabolism - extensive
Term
chloropheniramine
Definition
Class: antihistamine, H1 antagonist, 1st gen

Mechanism: antagonist at H1 receptors, some antimuscarinic activity

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp, sleep aid, prophylaxis and tx motion sickness, TX N AND V

Adverse effects: "drowsiness, sedation"; dizziness, lassitude, fatigue, nervousness, insomnia, tremor, loss of appetite, nausea, vomit, hypersensitivity rxn, dry mouth, blurred vision, urinary retention

Pharmacokinetics:
Absorption - well in GI
Distribution - hihgly lipid soluble, easy to CNS
Metabolism - extensive
Term
pyrilamine
Definition
Class: antihistamine, H1 antagonist, 1st gen

Mechanism: antagonist at H1 receptors, some antimuscarinic activity

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp, sleep aid, prophylaxis and tx motion sickness

Adverse effects: "drowsiness, sedation"; dizziness, lassitude, fatigue, nervousness, insomnia, tremor, loss of appetite, nausea, vomit, hypersensitivity rxn, dry mouth, blurred vision, urinary retention

Pharmacokinetics:
Absorption - well in GI
Distribution - hihgly lipid soluble, easy to CNS
Metabolism - extensive
Term
cetirizine
Definition
Class: antihistamine, H1 antagonist, 2nd gen

Mechanism: antagonist at H1 receptors

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp

Adverse effects: less sedation and drowsiness, (no antimuscarinic)

Pharmacokinetics:
Absorption - well in GI
Distribution - not much to CNS, ionized at pH7.4, highly bound to albumin
Metabolism - P450 system
Term
loratadine
Definition
Class: antihistamine, H1 antagonist, 2nd gen

Mechanism: antagonist at H1 receptors

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp

Adverse effects: less sedation and drowsiness, (no antimuscarinic)

Pharmacokinetics:
Absorption - well in GI
Distribution - not much to CNS, ionized at pH7.4, highly bound to albumin
Metabolism - P450 system
Term
desloratadine
Definition
Class: antihistamine, H1 antagonist, 2nd gen

Mechanism: antagonist at H1 receptors

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp

Adverse effects: less sedation and drowsiness, (no antimuscarinic)

Pharmacokinetics:
Absorption - well in GI
Distribution - not much to CNS, ionized at pH7.4, highly bound to albumin
Metabolism - P450 system
Term
fexofenadine
Definition
Class: antihistamine, H1 antagonist, 2nd gen

Mechanism: antagonist at H1 receptors

Indication: acute allergic rxn, reduce itching, diminish cold and flu symp

Adverse effects: less sedation and drowsiness, (no antimuscarinic)

Pharmacokinetics:
Absorption - well in GI
Distribution - not much to CNS, ionized at pH7.4, highly bound to albumin
Metabolism - P450 system
Term
sumatriptan
Definition
Class: migraine,

Mechanism: activates subset of 5HT receptors; direct vasoconstrictor on intracranial blood vessels, presynaptic inhibition on sensory neurons

Indication: abortive drug class of choice for migraine +/- aura [not prophylaxis or long-term tx]

Contraindication: hx of ischemic or vasospastic CAD, cerebrovascular or periph vasc disease, uncontrolled hypertension, taking MAO inhibitors

Adverse effects: nausea, malaise, dizziness, weakness, dry mouth, paresthesia, pain at injection site; rare: serious CV complications (coronary artery spasm, ischemia, arrhythmias)

Pharmacokinetics:
Absorption - subq injection, oral, nasal spray; 15-40% bioavailability orally
Onset: 10-15min after injection or nasal spray
Term
naratriptan
Definition
Class: migraine,

Mechanism: activates subset of 5HT receptors; direct vasoconstrictor on intracranial blood vessels, presynaptic inhibition on sensory neurons

Indication: abortive drug class of choice for migraine +/- aura [not prophylaxis or long-term tx]

Contraindication: hx of ischemic or vasospastic CAD, cerebrovascular or periph vasc disease, uncontrolled hypertension, taking MAO inhibitors, SEVERE RENAL OR HEPATIC DISEASE

Adverse effects: nausea, malaise, dizziness, weakness, dry mouth, paresthesia, pain at injection site; rare: serious CV complications (coronary artery spasm, ischemia, arrhythmias)

Pharmacokinetics:
Absorption - subq injection, oral, nasal spray; 15-40% bioavailability orally
Onset: 10-15min after injection or nasal spray
Term
almotriptan
Definition
Class: migraine,

Mechanism: activates subset of 5HT receptors; direct vasoconstrictor on intracranial blood vessels, presynaptic inhibition on sensory neurons

Indication: abortive drug class of choice for migraine +/- aura [not prophylaxis or long-term tx]

Contraindication: hx of ischemic or vasospastic CAD, cerebrovascular or periph vasc disease, uncontrolled hypertension, taking MAO inhibitors

Adverse effects: nausea, malaise, dizziness, weakness, dry mouth, paresthesia, pain at injection site; rare: serious CV complications (coronary artery spasm, ischemia, arrhythmias)

Pharmacokinetics:
Absorption - subq injection, oral, nasal spray; 15-40% bioavailability orally
Onset: 10-15min after injection or nasal spray
Term
rizatriptan
Definition
Class: migraine,

Mechanism: activates subset of 5HT receptors; direct vasoconstrictor on intracranial blood vessels, presynaptic inhibition on sensory neurons

Indication: abortive drug class of choice for migraine +/- aura [not prophylaxis or long-term tx]

Contraindication: hx of ischemic or vasospastic CAD, cerebrovascular or periph vasc disease, uncontrolled hypertension, taking MAO inhibitors

Adverse effects: nausea, malaise, dizziness, weakness, dry mouth, paresthesia, pain at injection site; rare: serious CV complications (coronary artery spasm, ischemia, arrhythmias)

Pharmacokinetics:
Absorption - subq injection, oral, nasal spray; 15-40% bioavailability orally
Onset: 10-15min after injection or nasal spray
Term
zolmitraptan
Definition
Class: migraine,

Mechanism: activates subset of 5HT receptors; direct vasoconstrictor on intracranial blood vessels, presynaptic inhibition on sensory neurons

Indication: abortive drug class of choice for migraine +/- aura [not prophylaxis or long-term tx]

Contraindication: hx of ischemic or vasospastic CAD, cerebrovascular or periph vasc disease, uncontrolled hypertension, taking MAO inhibitors

Adverse effects: nausea, malaise, dizziness, weakness, dry mouth, paresthesia, pain at injection site; rare: serious CV complications (coronary artery spasm, ischemia, arrhythmias)

Pharmacokinetics:
Absorption - subq injection, oral, nasal spray; 15-40% bioavailability orally
Onset: 10-15min after injection or nasal spray
Term
topiramate (migraine)
Definition
Class: migraine, anticonvulsant

Mechanism: decrease frequency of migraines

Indication: migraine prophylaxis
Term
ergpotamine
Definition
Class: migraine

Mechanism: agonist and antagonist at many receptors; agonist at 5HT receptors

Indication: migraines

Contraindicated: pregnancy (uterine stimulant and restrict blood flow), CAD or PVD, hypertension, liver or renal disease

Adverse effects: nausea, vasoconstriction with ischemia, leg weakness, muscle pain
Term
dihydroergotamine
Definition
Class: migraine

Mechanism: agonist and antagonist at many receptors; agonist at 5HT receptors

Indication: migraines

Contraindicated: pregnancy (uterine stimulant and restrict blood flow), CAD or PVD, hypertension, liver or renal disease

Adverse effects: nausea, vasoconstriction with ischemia, leg weakness, muscle pain
Term
methysergide
Definition
Class: migraine

Mechanism: agonist and antagonist at many receptors; agonist at 5HT receptors; ANTAGONIST AT 5HT(2A/2C) RECEPTOR

Indication: migraine prophylaxis

Contraindicated: pregnancy (uterine stimulant and restrict blood flow), CAD or PVD, hypertension, liver or renal disease

Adverse effects: nausea, vasoconstriction with ischemia, leg weakness, muscle pain; long-term: RETROPERITONEAL, CARDIAC, OR LUNG FIBROSIS (USE <6MO ONLY)
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