P H R M A C O L O G Y - NOTE 15 Anit-migraine Drugs

ANTI-MIGRINE DRUGS

Acute Attack
Mild to
Moderate

NSAIDs

Prophylaxis

Moderat to
Sever

Anti- emetics

prokinetic

adrenergic
blockers

Specific drug

Diclofenac

5-HT Agonist

P Agonest for Adrenceptors & 5HT R

Ca channel
blockers

5-HT2
antagonist

Propranolol

Flunarizine

Pizotifen

Metoprolol

Nicardipine

Cyprohepatadine

5HT2 antagonist
/partial agonist

Methysergide

Other

Amitryptyline

Aspirin

Diphenhydramine

Metocloperamide

Sumatripan

Paracetamol

Promethazine

Domperidone

Almotriptan

Nadolol

Nifedipine

Sertraline

Ibuprofen

Naratriptan

Atenolol

Nimodipine

Fluoxetine

Indomethacin

Pizatriptan

Timolol

Verapamil

Clonidine

Naproxene

Zolmitriptan

Ergotamine

Imipramine

Valporate

Opioids

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P H R M A C O L O G Y - NOTE 15 Anit-migraine Drugs

Acute attack of Migraine
Aspirin
Paracetamol
Ibuprofen
Indomethacin
Naproxene
Opioids

USES

SIDE EFFECT

acute migraine attack.

Refractory cases of
acute attack of
migraine(rarly)

Efficient use of analgesic &

antiemetic is sufficient for the
majority of ACUTE ATTACKS

Prevent vomiting.

Promethazine
Metocloperamide
Domperidone

Almotriptan
Naratriptan
Pizatriptan
Zolmitriptan
Ergotamine

P Agonest for -Adrenceptors & 5-HT R

5-HT Agonist

ACTION
Analgesic.

Given parentrally (I.V. or I.M.).

Diphenhydramine

Diclofenac
Sumatripan

Specific drug for acute attake

PHARMACOKINETIC
Given orally.
they must be given early to be absorbed before
there is vomiting.

Given by I.V. injection.

Given as rectal suppositories for vomiting can
be tried

Given by oral route or S.C. injection.

Fast absorbtion.
Bioavailabilty by s.c. route is 96%
Dose not cross BBB.
Plasma t1/2 is 2 hours.

they are congeners of Sumatriptan.

improved pharmacokinetic
better Bioavailability.
better and longer duration.
Ergotamine tartrate

Given by o Entral route (oral, sublingual, rectal).

o Parentral route (inhaler).
rectal route is preferred ???.
caffeine facilitates absorption of ergot alkaloid.

They promote gastric emptying,

So, enhances absorption of
analgesics.

With very severe

vomiting.

stimulate 5-HT1 R on presynaptic endings of V cn.

inhibit releasing of
vasodilators .
selectively stimulates
5HT1B/1D R in cranial BV,
constrict them.

acute severe migraine

attack(1st line).
NOT used with
IHD.
unstable angina.
previous MI

stimulate 5-HT1 R on pre-synaptic

endings of V cn.
inhibit releasing of
vasodilators .

Malaise ,fatigue.
Sedation.
Dizziness, vertigo, nausea & vomiting.
feeling of chest pressure, tightness & pain.
CARDIAC ARRHYTHMIA & myocardial infarction.
due to coronary artery spasm.

Less side effects.

Reduce cardiac side effects.

+ effects
on CNS

NSAIDs
Anti- emetics
prokinetic

Moderat to Sever
attack

Mild to Moderate
attack

DRUG

Migrine (high specific).

Paresthesiae in hands & feet.

Peripheral ischaemia.
Peripheral GANGRENE with overdose.
Precipitate angina pectoris.
Fetal damage.

It metabolized in the liver.

t is 2 hrs
DOSE.

o Tablet (1mg + Caffeine 100mg).

o 1-2 tab. at onset ,then 1 tab/ 30min.
o NO > 6 mg/attack & NO >10 mg/wk.
For severe attack, it ginen may be IM/IV injct.
Dihydroergotamine o For intractable migraine.
o Given by IV inj.(0.5-1mg)

NOT used with disease

of:
Coronary BV.
Peripheral BV.

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P H R M A C O L O G Y - NOTE 15 Anit-migraine Drugs

Prophylaxis drugs for Migrine.
DRUG

Other

5HT2 antagonist
/partial agonist

5-HT2
Ca channel blockers
antagonist

adrenergic blockers

Propranolol

PHARMACOKINETIC

PROPRANOLOL (effect ,
also prevent migraine ).

Metoprolol
Nadolol
Atenolol
Timolol
Flunarizine
Nicardipine
Nifedipine
Nimodipine
Verapamil
Pizotifen
Cyprohepatadine
Methysergide

Amitryptyline
Imipramine
Sertraline
Fluoxetine
Clonidine
Valporate

effective in about 60% patients.

ACTION

USES

the d-isomer part of structure lacks

blocking action;
Alter the permeability of the
membrane.

They are effective and widely used.

Fatigue.
Broncho-constriction.

Block Ca channel.

effective in the preventive treatment

of Migraine

They are RARELY used

antagonize5-HT2 receptors.
Atropine like action.
Antagonize 5-HT2 R & H 1 R.
Block Ca channels
It is 5HT2 antagonist /partial agonist

SIDE EFFECT

Weight gain.
Anti-cholinergic side effects.
Sedation.
weight gain.
Serious Toxicities like;
o RETROPERITONEAL
obstruction to the Ureters.
o Subendocardial, Pericardial or Pleural fibrosis.
Nausea, vomiting & diarrhoea.

effective for the PROPHYLAXIS of

migraine in some patients.

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