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Pharmacology

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Autonomic Nervous Systems

Question
52 out of 75
 

Used for the treatment of migraine, the triptans act through: (AIIMS Nov 2009)



A 5HT-1A
B 5HT-1B

C 5HT-1F
D 5HT-3

Ans. B 5HT-1B

Triptans act by activating 5-HT1b/1d. sumatriptan was the first triptan to have been used clinically. After that several drugs have been released and these include elmetriptan, zolmitriptan, elitidan and rizatriptan. Since these receptors are also present on coronaries; therefore contraction of cerebral vessels may be accompanied by constriction of coronaries leading to coronary vasospasm. Hence the drug is contraindicated in coronary artery disease. Sumatriptan and allied drugs are the drugs of choice for acute attack of migraine. Bioavailability of these drugs is poor.

Table: Acute Migraine-Specific Agents

5-HT1 Agonists

Selective

Nonselective

Sumatriptan

Ergotamine

Zolmitriptan

Dihydroergotamine

Naratriptan

Rizatriptan

Eletriptan

Almotriptan

Frovatriptan

Table 2.Pharmacokinetics of Triptans (http://www.ouch-us.org/medications/triptans.htm)

Tmax (hrs)

Half-life (hrs)

Oral bioavailability

Lipophilicity

Metabolism

Sumatriptan

2 (2.5)*

2.5

15%

-1.3

MAO

Zolmitriptan

2 (2.5)*

3

40%

-0.7

MAO

Naratriptan

2-3 (3-4)*

6

70%

-0.2

Cytochrome P450 MAO

Rizatriptan

1-1.5

2-3

45%

-0.7

MAO

Eletriptan

1.5 (2.8)*

4-5

50%

+0.5

Cytochrome P450

Almotriptan

1.4-3.8

3.2-3.7

69%

-0.35

Cyp3A4 , Cyp2D6 MAO

Frovatriptan

2-3

25

30% (F)
20% (M)

Cyp1A2

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