Antimigraine Drugs; Uses/Indications, Side Effects, Interactions

Antimigraine drugs are the groups of drug that are used for treatment or prevention of a pain?, nausea?, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine?. A migraine is a primary pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache? disorder characterized by recurrent headaches that are moderate to severe. Typically, the headaches affect one half of the head, are pulsating in nature, and last from two to 72 hours. Associated symptoms may include nausea?, vomiting?, and sensitivity to light, sound, or smell. The pain? is generally made worse by physical activity. Up to one-third of people have an aura: typically a short period of visual disturbance that signals that a pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache? will soon occur. Occasionally, an aura can occur with little or no pain? in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache? following it.

Classifications / Types of Antimigraine

Mechanism of Action of Antimigraine

Their action is attributed to their agonist effects on serotonin 5‑HT_1B and 5‑HT_1D receptors in blood vessels (causing their constriction) and nerve endings in the brain, and subsequent inhibition of pro-inflammatory neuropeptide release, including CGRP and substance P. Triptans are selective agents for 5-HT_1B and 5-HT_1D and have low or even no affinity for other types of 5-HT receptors.

5-HT receptors are classified into seven different families named 5-HT₁ to 5-HT₇. All receptors are G protein-coupled receptors with seven transmembrane domains with the one exception of 5-HT₃ receptor which is a ligand-gated ion channel. There is a high homology in the amino acid sequence within each family. Each family couples to the same second messenger systems. Subtypes of 5-HT₁ are the 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1E, and 5-HT_1F receptors. All 5-HT_1D receptors are coupled to inhibition of adenylate cyclase. 5-HT_1Band 5-HT_1D receptors have been difficult to distinguish on a pharmacological basis. After cloning two distinct genes for 5-HT_1B and 5-HT_1D receptors, a better insight into distribution and expression in different tissues was gained, except in brain tissue where they are overlapping in several areas

Most mammalian species, including humans, have 5-HT_1D binding sites widely distributed throughout the central nervous system. 5-HT_1D receptors are found in all areas of the brain but they differ in quantity at each area. An important initiator of head pain? is suggested to be the activation of trigeminovascular afferent nerves which upon activation releases neuropeptides such as CGRP, substance P and neurokinin A. Also they are thought to promote neurogenic inflammatory response important for sensitization of sensory afferents, and also transmission and generation of head pain centrally. 5-HT_1D has been found responsible for inhibition of neurogenic infection?, or irritation, often causing pain?, swelling?, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation? upon administration with sumatriptan and other related compounds that act on prejunctional 5-HT_1D receptors.

All triptans, like the older drug dihydroergotamine, have agonistic effects on the 5-HT_1D receptor. Comparison of sumatriptan and dihydroergotamine showed that dihydroergotamine has high affinity and sumatriptan has a medium affinity for 5-HT_1D. Triptans have at least three modes of action. These antimigraine mechanisms are:

1. vasoconstriction of pain?-producing intracranial extracerebral vessels by a direct effect on vascular smooth muscle. Sumatriptan and rizatriptan have been shown to cause vasoconstriction in the human middle meningeal arteries.
2. inhibition of vasoactive neuropeptide release by trigeminal terminals innervating intracranial vessels and the dura mater. The trigeminocervical complex has 5-HT_1D receptors that bind dihydroergotamine and triptans in humans. Rizatriptan has been shown to block dural vasodilation and plasma protein extravasation by inhibiting the release of CGRP via activation of receptors on preganglionic trigeminal sensory nerves terminals. Sumatriptan is shown to inhibit potassium stimulated CGRP secretion from cultured trigeminal neurons in a dose dependent manner and may also inhibit the release of substance P.
3. inhibition of nociceptive neurotransmission within the trigeminocervical complex in the brainstem and upper cervical? spinal column. Rizatriptan has central trigeminal antinociceptive activity.

Other possibilities of triptans in antimigraine effects are modulation of nitric oxide-dependent signal transduction pathways, nitric oxide scavenging in the brain, and sodium-dependent cell metabolic activity.

Indications of Antimigraine

• Migraines

Contra-Indications of Antimigraine

• Migraine Headache with Temporary Paralysis of One Side
• Severe uncontrolled high blood pressure
• Transient ischaemic attack(TIA), peripheral vascular disease, severe hepatic impairment, concomitant administration of ergotamine, ergotamine derivatives
• Heart attack
• Myocardial infarction, angina pectoris, documented silent ischaemia, Prinzmetal’s angina
• Type of angina where Chest Pain Occurs at Rest
• Coronary artery disease
• Disease of Inadequate Blood Flow to the Heart Muscle ,abnormal heart rhythm
• Occasional Numbness or Tingling of Fingers and Toes
• Peripheral vascular disease
• Insufficiency of the vascular system of the intestine
• Severe renal? impairment
• Family History of inadequate blood flow to the heart muscle
• Increased cardiovascular event risk
• Allergies to triptans-5-HT1 Antimigraine Agents

Do not take almotriptan within 24 hours before or after using another pain?, nausea?, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine? headache? medicine

Side Effects of Antimigraine

The most common

• Nausea/vomiting
• sleepiness
• feeling of pain or tightness in your jaw, neck, or throat;
• chest pain or heavy feeling, pain? spreading to the arm or shoulder, sweating, general ill feeling;
• sudden numbness or weakness, 
• Confusion, problems with vision, speech, or balance;
• headache
• dry mouth
• dizziness
• Constipation
• Weight gain/loss

More common

• Abdominal or stomach pain, discomfort, or pain? when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।" data-rx-term="tenderness" data-rx-definition="Tenderness means pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।">tenderness?
• chills or fever
• difficulty with moving
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• discomfort in arms, shoulders, neck or upper back
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• rust colored urine
• decreased amount of urine

Rare

• Anxiety
• change in vision
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain?
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities

Drug Interactions of Antimigraine

Antimigraine drugs may interact with the following drug, supplements, & may change the efficacy of the drug

• amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
• atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
• azathioprine
• barbiturates (e.g., butalbital, pentobarbital phenobarbital)
• antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, , quetiapine, risperidone)
• beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• ergotamine-containing or ergot-type medications (e.g., dihydroergotamine, methysergide)
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• metoclopramide
• protease inhibitors (e.g., indinavir, lopinavir, ritonavir)
• selective norepinephrine reuptake inhibitors (SNRIs; e.g., venlafaxine)
• selective serotonin receptor agonists (SSRIs; e.g., fluoxetine, fluvoxamine, paroxetine, sertraline)
• trimethoprim
• valproic acid
• warfarin

References