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Pharmacology .. Anit-migraine Drugs
1. P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
ANTI-MIGRINE DRUGS
Acute Attack Prophylaxis
Mild to Moderat to β adrenergic Ca channel 5-HT2 5HT2 antagonist
Specific drug /partial agonist Other
Moderate Sever blockers blockers antagonist
P Agonest for α-
NSAIDs Anti- emetics prokinetic Diclofenac 5-HT Agonist Adrenceptors & 5- Propranolol Flunarizine Pizotifen Methysergide Amitryptyline
HT R
Diphenhydr- Metocloper- Cyprohepata-
Aspirin Sumatripan Ergotamine Metoprolol Nicardipine Imipramine
amine amide dine
Paracetamol Promethazine Domperidone Almotriptan Nadolol Nifedipine Sertraline
Ibuprofen Naratriptan Atenolol Nimodipine Fluoxetine
Indomethacin Pizatriptan Timolol Verapamil Clonidine
Naproxene Zolmitriptan Valporate
Opioids
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2. P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
Acute attack of Migraine
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Aspirin Given orally. Analgesic. acute migraine attack.
Mild to Moderate
Paracetamol they must be given early to be absorbed before
NSAIDs
Ibuprofen there is vomiting.
attack
Indomethacin
Naproxene
Opioids Given parentrally (I.V. or I.M.). Refractory cases of
acute attack of
Efficient use of analgesic &
migraine(rarly)
antiemetic is sufficient for the
Diphenhydramine Prevent vomiting.
Anti- emetics
majority of ACUTE ATTACKS
Moderat to Sever
Promethazine
attack
Metocloperamide Given by I.V. injection. They promote gastric emptying, With very severe
prokinetic
So, enhances absorption of vomiting.
Domperidone Given as rectal suppositories for vomiting can analgesics.
be tried
Diclofenac
Sumatripan Given by oral route or S.C. injection. stimulate 5-HT1 R on pre- acute severe migraine Malaise ,fatigue.
Fast absorbtion. synaptic endings of V cn. attack(1st line). Sedation.
Bioavailabilty by s.c. route is 96% inhibit releasing of Dizziness, vertigo, nausea & vomiting.
Dose not cross BBB. vasodilators . NOT used with feeling of chest pressure, tightness & pain.
5-HT Agonist
Plasma t1/2 is 2 hours. selectively stimulates IHD. CARDIAC ARRHYTHMIA & myocardial infarction.
5HT1B/1D R in cranial BV, unstable angina. due to coronary artery spasm.
constrict them. previous MI
Almotriptan they are congeners of Sumatriptan. Less side effects.
Specific drug for acute attake
+ effects
on CNS
Naratriptan improved pharmacokinetic Reduce cardiac side effects.
Pizatriptan better Bioavailability.
better and longer duration.
Zolmitriptan
Ergotamine Ergotamine tartrate stimulate 5-HT1 R on pre-synaptic Migrine (high specific). Paresthesiae in hands & feet.
Given by o Entral route (oral, sublingual, rectal). endings of V cn. Peripheral ischaemia.
P Agonest for α-Adrenceptors & 5-HT R
o Parentral route (inhaler). inhibit releasing of Peripheral GANGRENE with overdose.
rectal route is preferred ???. vasodilators . Precipitate angina pectoris.
caffeine facilitates absorption of ergot alkaloid. Fetal damage.
It metabolized in the liver.
t ½ is 2 hrs NOT used with disease
DOSE. of:
o Tablet (1mg + Caffeine 100mg). Coronary BV.
o 1-2 tab. at onset ,then 1 tab/ 30min. Peripheral BV.
o NO > 6 mg/attack & NO >10 mg/wk.
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For severe attack, it ginen may be IM/IV injct.
Dihydroergotamine o For intractable migraine.
o Given by IV inj.(0.5-1mg)
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3. P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
Prophylaxis drugs for Migrine.
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Propranolol • PROPRANOLOL– (effect , the d-isomer part of structure lacks β They are effective and widely used. Fatigue.
also prevent migraine ). blocking action; Broncho-constriction.
β adrenergic blockers
Alter the permeability of the
membrane.
Metoprolol
Nadolol
Atenolol
Timolol
Block Ca channel.
Ca channel blockers
Flunarizine effective in the preventive treatment
Nicardipine of Migraine
Nifedipine
Nimodipine
Verapamil
Pizotifen antagonize5-HT2 receptors. They are RARELY used Weight gain.
antagonist
Atropine like action. Anti-cholinergic side effects.
5-HT2
Cyprohepatadine Antagonize 5-HT2 R & H 1 R. Sedation.
Block Ca channels weight gain.
Methysergide effective in about 60% patients. It is 5HT2 antagonist /partial agonist Serious Toxicities like;
5HT2 antagonist
/partial agonist
o RETROPERITONEAL
obstruction to the Ureters.
o Subendocardial, Pericardial or Pleural fibrosis.
Nausea, vomiting & diarrhoea.
Amitryptyline effective for the PROPHYLAXIS of
Imipramine migraine in some patients.
Other
Sertraline
Fluoxetine
Clonidine
Valporate
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