Handbook of clinical drug data.pdf - Me and My Life

6 ANALGESIC AND ANTI-INFLAMMATORY DRUGSmacrolides (especially erythromycin and troleandomycin) can inhibit the metabolismof ergot alkaloids.Notes. The stimulant action of preparations containing caffeine can keep patientsfrom the beneficial effects of sleep. Caffeine, however, can improve dissolution ofthe oral formulation. Ergotamine is commonly used for abortive therapy of migraineand provides relief in 50–90% of patients. 7 Aspirin (650 mg) or naproxen(750–1250 mg/day) might be effective in aborting migraine headache in mildcases or in patients who cannot take ergotamine. OTC products containing aspirin,acetaminophen, and caffeine (Excedrin Migraine) or ibuprofen (Advil Migraine,Motrin Migraine) have FDA approval for mild to moderate migraine. Prescriptioncombination products such as Midrin and Fiorinal might be useful, but overuseof any antimigraine combination product can lead to rebound headache. NSAIDsare useful for prophylaxis against menstrual-related migraines when taken duringthe perimenstrual period. Butorphanol spray might be beneficial for patients withinfrequent, severe headaches who cannot tolerate ergot products or triptans, butfrequent use can cause dependency. The -blockers propranolol and timolol areapproved by the FDA for migraine prophylaxis, but other -blockers without intrinsicsympathomimetic activity (eg, atenolol, nadolol) are also useful. Verapamilcan prevent migraines in some patients but can take several months to reachmaximum effectiveness. Tricyclic antidepressants (eg, amitriptyline, nortriptyline)have been more successful in migraine prophylaxis than SSRIs. Divalproexhas been used successfully for prophylaxis. Consider frequency of attacks(more than 2/month), co-morbid conditions, and side effects when choosing prophylactictherapy. Effective doses for migraine prophylaxis drugs are usuallylower than those used for other indications. 11METHYSERGIDE MALEATESansertPharmacology. Methysergide is a semisynthetic ergot alkaloid, thought to actcentrally as a serotonin agonist and to inhibit blood vessel permeability to humoralfactors that affect pain threshold. Unlike other ergots, methysergide doesnot inhibit reuptake of norepinephrine and has minimal oxytocic, vasoconstrictor,and -adrenergic blocking effects. Because of its toxicity, methysergide is usuallyused only after other prophylactic measures have failed.Adult Dosage. PO for migraine or cluster headache prophylaxis 4–8 mg/daywith food. A drug-free interval of 3–4 weeks must follow each 6-month course;however, reduce the dosage gradually to avoid rebound headache.Dosage Forms. Tab 2 mg.Pharmacokinetics. Methysergide undergoes extensive liver metabolism tomethylergonovine, a compound with greater activity and a longer eliminationhalf-life than the parent drug (3.5 hr vs 1 hr). About 56% of an oral dose is eliminatedin the urine as unchanged drug and metabolites.Adverse Reactions. Insomnia, postural hypotension, nausea, vomiting, diarrhea,and peripheral ischemia occur frequently. Occasionally, heartburn, peripheraledema, rash, or arrhythmias occur. Rarely, mental depression occurs. Long-term(>6 months) therapy can cause retroperitoneal and pleuropulmonary fibrosis and