Agents for Migraine include

Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan

Refer - Sumatriptan 

Drug interaction - Potent CYP3A4 inhibitors e.g ketoconazole,itraconazole, nefazodone, troleandomycin, clarithromycin, rotonavir, nelfinavir with almotriptan incr coadmin. of almotriptan and ketoconazole (400mg/day for 3 days) resulted Electriptan in an increase in AUC and maximal plasma concentration of almotriptan. The AUC and Cmax of eletriptan are increased with coadmin.. Do not use electriptan within 72 hurs of treatment with potent CYP3A4 inhibitors 

MAOIs with

Almotriptan incr use of certain 5-HT1 agonists cocurrently with or within 2 weeks following Rizatriptan discontinuing an MAOI is contraindicated. It is necessary to use such Sumitriptan agents together, naratriptan, eletriptan, and fravotriptan appear to be Zolmitriptan less likely to interact with MAOIs. 

Frovatriptan, Naratriptan, Rizatriptan Sumitriptan, Zolmitriptan with SSRIs incr there have been reports of weakness, hyperflexia, and incordination with Fluoxetine, combined use of SSRIs. It is concomitant use is clinically warranted, fluvoxetine observe the patient carefully. No interaction was observed when paroxetine, serataline riztriptan was coadministerd with paroxetine. fluoxetine had not effect on almotriptan, but clearance, Cmax increased by 18%.

Acute treatment of migraine 

Agents for Migraine include- Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan

Refer -Sumatriptan

Malaise, fatigue, diziness, drowsiness, nausea Pain or sensation or warmth Heavines or pressure in any part of the body including the throat or chest Rarely- ischarmic colitis and serious cardiac events Serious coronary vasospasm , transient mycardial ischemia, ventricullar fibrillation/ tachycardia, amd MI have been associated with 5-HT1 agonists. Oral - these agents have been well tolerated. Across all doses most adverse reactions have been mild and transcient aand did not lead to long lasting effects. ----------------------------------- Atypical sensations- warm/cold temperature sensations, strange feeling and burning/stinging sensation Cardiovascular- abnormal ECG, QT prolongation, ST/T wave abnormalities, premature ventricular contractions, atrial flutter/fibrillation, increased blood pressure, palpitations, syncope, tachyarrhythmias, bradycardia, heart murmurs,hypotension, varicosities. CNS- vertigo.anxiety, cognitive function disorders, depressive disorders, equillibrium disorders, sleep disoders, tremors.aggresion, agitation, compressed nerve symptoms, confusion, decreased consciousness, dreams, hallucinations, hostility, hyperactivity. Dermatologic- pruritus, skin rashes, urticaria, allergic skin, sweating, urticaria, acne, allergic skin reactions, dermititis, folliculitis, hair loss, photodermitis, photosensitivity, skin erythemia, skin flakiness/ dryness. GI- hyposalivation, vomiting, constipation, diarrhea/discomfort/pain, dyspeptic symptoms, gastroenteritis, abnormal bilirubin levels, abnormal liver function tests, altered sense of taste, esophagitis, gastric ulcers, gastritis, hemorrhoids, oral itchng and irritation, regurgitation and reflux, salivary gland inflammation. GU- bladder inflammation diuresis, ployuria, breast discharge, decreased libido, endometruium disorders,lumps in breast, urinary incontinence, urinary tract hemorrhage, urinary urgency, vaginal inflammation. Hematologic- increased white cells, anemia, purpura, quantitative red or hemoglobin defects thrombocytopenia Metabolic nutritional - dehydration, fluid retention, thirst, glycosuria, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypothyroidism, ketonuria. Musculoskeltal- pressure/tightness/heaviness sensations, arthalgia, articular rheumatism, joint/muscle stiffness, muscle cramps, muscle spasms, muscle pain, rigidity, tightness. Respiratory- bronchitis, cough, pneumonia, airway obstruction/constriction, asthma, pleuritis, tracheitis Special senses- photophobia, blurred vision, aphasia, difficulty focussing, dry eyes, eye haemorrhage ,eye pain, /discomfort, sensation of eye pressure Ear , nose and throat - ear, nose throat infections, photophobia, sinusitis, tinnitus, upper respiratory tract inflammation., allergic rhinitis, ear/nose / throat hemorrhage Miscellaneous- allergic reactions, allergies, chills, descriptions of odour or taste, edema, fever, swelling, mobility disorders, spasms.

Injectable preparation used IV because of potential to cause coronary vasospasm, patients wit ischemic heart disease ( angina pectoris ) history of MI , strokes, ischemic attacks TIAs or documented silent ischemia Prinzmetal variant angina or significant underlying cardiovascular disease Concurrent use of ( use within 24 hours of ) ergot containg prepn or ergot type medications such as dihydroergotamine or methysergide Concurrent monoamine oxidase inhibitors MAOI therapy ( or within 2 weeks of discontinuing an MAOI ( except eletriptan ) Naratriptan and sumitriptan - cerbrovascular or peripheral vascular syndromes, severe impairment, ( child Pugh grade C) severe renal impairment (Ccr less than 15mL/min ( naratriotan only) Frovatriotan and eletriptan - peripheral vascular disease Eletriptan - severe hepatic impairment Warnings/precautions- Risk of myocardial ischemia or MI and other adverse cardiac events- because of the potential of these compounds to cause coronary vasospasm, do not give these agents to patients with documented ischemic or vasopastic coronary artery disease It is strongly recommended that that 5-HT1 agonists not be given to patients in whom unrecognized coronary artery disease CAD is predicted by the presence of risk factors eg. hypertension, hyperchloesrolemia, smoking, obesity, diabetes, strong family history of CAD, female with surgical or physilogical menopause or male older than 40 years of age) unless a cardiovascular evaluation provides satisfactory clinical evidence that the patient is reasonably free of coronary artery and ischemic myocardial disease or significant underlying cardiovascular disease Zolmitriptan- there is a report of at least 1 patient experiencing coronary vasospasm without the history of cardiac disease and with documented history of absence of CAD. Patients with symptomatic Wolff- Parkinson -White syndrome or arrhthmias associated with cardiac accessory conduction pathway disorders should not receive zolmitriptan Cardiac events and fatalities associated with 5-HT1 agonists- serious adverse cardiac events including acute MI , life threatening disturbances of cardiac rhythm, and death have been reported within few hours following admin. of 5- HT1 agonists. Considering the use of 5 - HT1 agonists in patients with migraine , the incidence of these events is extremely low. Cerbrovascular events and fatalities with 5-HT1 agonists- cerebral hemorrhage , subarachnoid hemorrhage , stroke, and other cerebrovascular events have been reported in patients treated with 5-Ht1 agonists and some have resulted in fatalites. It should be noted that patients with migraine may be at increased risk of certain cerebrovacular events eg. stroke, hemorrhage, TIA Other vasospasm related events- 5-HT1c agonists may cause vasospatic reactions other than coronary artery vasospasm . Peripheral vascular ischemiand colonic ischemia with abdominal pain and bloody diarrhea have been reported with 5-HT1 agonists. Increase in blood pressure- significant increase in blood pressure including hypertensive crisis have been reported on rare occassions in patients with a history of with or without hypertension trreated with 5HT1 agonists. 5-HT1 agonists are contraindicated in patients with uncontrolled hypertension. Renal function impairment- Use rizatriptan and sumitriptan with caution in dialysis patients becausec of decrease in clearance Hepatic function impairment- Administer with caution to patients with diseases that may alter the absorption,metabolism, or excretion of drugs. Phtosensitivity- Photosenrization may occur. Caution patients to take protective measures Use during pregnancy only if the potential benefits justifies the potential risk to the fetus Lactation- Sumatriptan and eletriptan are excreted in human breast milk. Lactating rats dosed with zolmitriptan had milk levels equivalent to maternal plasma levels at 1 hour and 4 times higher than plasma levels at 4 hours Naratriptan -related material is excreted in milk of rats. Rizatriptan is extensively excreted in rat milk at a level 5-fold or greater than matenal plasms levels Frovatriptan and its metabolites are excreted in the milk of lactating rats with maximum concentration being 4 fold than seen in blood. Excercise caution when administering to a nursing woman Children- safety and efficacy have not beenestablished. Elderly- Pharmacokinetics disposition of 5-HT1 agonists in the elderly is similar to that seen in younger adults.

Dosage-

1 tab at onset of attack. If symptoms recur a repeat dose may be given after min. 4 hours.

Maximum 5mg in 24 hours patients who fail respond initially should not receive a repeat dose for the same attack.

Patients over 65 years and below 18 years not recommended

 Agents for Migraine include- Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan

Refer Almotriptan

Pharmacology- Sumatriptan, naratriptan, zolmitriptan, rizatriptan, frovatriptan, eletriptan and almotriptan are selective 5-hydroxytryptamine1 (5-HT1 or serotonin ) receptor agonists

Pharmacokinetics- RENAL FUNCTION IMPAIRMENT -- Naratriptan - Clearance of naratriptan was reduced by 50% in patients with moderate renal impairment ( Ccr 18 to 39 mL/min. resultiing in an increase in mean half life from 6 hours ( healthy ) to 11 hours (range 7 to 20 hours). The mean Cmax was increased by approx 40%. Effects of severe renal impairment have not been assessed. HEPATIC FUNCTION IMPAIRMENT- liver plays an important role in presystemic clearance of 5-HT1 agonists. Accodingly the bioavailability may be markedly increased in patients with liver disease.

Food has significant effect on oral 5-HT1 agonists bioavailability, but delays sumatriptans Tmax by aaproximately 30 minutes and rizatriptans time to reach peak concentration by 1 hour. AUC and Cmax of eletriptan are increased approximately 20% to 30% following oral admin. of a high fat meal.

Pregnancy- There are no adequate and well controlled studies in pregnant women Use during pregnancy only if the potential benefits justifies the potential risk to the fetus

Lactation- Naratriptan -related material is excreted in milk of rats. Excercise caution when administering to a nursing woman

Children- safety and efficacy have not beenestablished.

Elderly- Pharmacokinetics disposition of 5-HT agonists in the elderly is similar to that seen in younger adults.