Serotonin 5-HT1-receptor agonists

Key examples

• Sumatriptan

 

Common indications

• In acute migraine with or without aura, serotonin 5-HT1-receptor agonists, often referred to as ‘triptans’, are effective at reducing the duration and severity of headache symptoms.

 

Mechanisms of action

• Serotonin 5-HT1-receptor agonists relieve the symptoms of acute migraine. 
• Although the exact mechanisms underlying migraines are not completely understood, dilatation of cranial blood vessels is thought to be important. 
• Triptans constrict cranial blood vessels and inhibit neurotransmission in the peripheral trigeminal nerve and in the trigeminocervical complex.

 

Important adverse effects

• Common adverse effects of triptans include pain or discomfort in the chest and throat, which can be intense but should resolve quickly. 
• Rarely, myocardial infarction has been reported. 
• Other common adverse effects include nausea and vomiting, tiredness, dizziness and transient high blood pressure.

 

Warnings

• Due to their vasoconstrictor properties it is important that patients with coronary artery disease (e.g. angina, myocardial infarction) and cerebrovascular disease (e.g. stroke) do not take these drugs due to the risk of acute vascular events. 
• Triptans should not be used in patients with hemiplegic or basilar migraines.

 

Important interactions

• Triptans may increase the risk of serotonin toxicity and serotonin syndrome when given in combination with and other serotonergic drugs, such as monoamine oxidase inhibitors, tramadol, selective serotonin reuptake inhibitors and tricyclic antidepressants.