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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