What Are the Different Types of Over-the-Counter Migraine Medications?

In recent years, new drugs for migraine have greatly improved the prognosis of patients, the most revolutionary of which is triptans. The triptans can selectively stimulate the 5HT1B / 1D receptors. The 5HT1 receptors can treat migraine in the following ways: Stimulation of 5-HT1B receptors has only slight contraction of blood vessels in physiological state, but it can Strongly contract the dilated cerebrovascular and meningeal vessels; By stimulating presynaptic 5-HT1D receptors of the trigeminal nerve, inhibiting the neurogenic inflammatory response and plasma extravasation of the dura mater can reduce the CGRP in the blood during migraine. Calcium gene-related peptide) content; Inhibit the trigeminal nucleus excitation by stimulating the 5-HT1B or 5-HT1D receptors on the brain stem.

In recent years, new drugs for migraine have greatly improved the prognosis of patients, the most revolutionary of which is triptans. The triptans can selectively stimulate the 5HT1B / 1D receptors. The 5HT1 receptors can treat migraine in the following ways: Stimulation of 5-HT1B receptors has only slight contraction of blood vessels in physiological state, but it can Strongly contract the dilated cerebrovascular and meningeal vessels; By stimulating presynaptic 5-HT1D receptors of the trigeminal nerve, inhibiting the neurogenic inflammatory response and plasma extravasation of the dura mater can reduce the CGRP in the blood during migraine. Calcium gene-related peptide) content; Inhibit the trigeminal nucleus excitation by stimulating the 5-HT1B or 5-HT1D receptors on the brain stem.

Drug Name

Triptans

Whether prescription drugs

Non-prescription drugs

Main indications

Migraine

Adverse reactions

Dry mouth, dizziness, dizziness, discomfort, fatigue,

Main medication contraindications

Coronary spasm or pulmonary hypertension

In recent years, new drugs for migraine have greatly improved the prognosis of patients, the most revolutionary of which is triptans.

(I) Action mechanism of triptans:

The triptans can selectively stimulate the 5HT1B / 1D receptors. The 5HT1 receptors can treat migraine in the following ways: Stimulation of 5-HT1B receptors has only slight contraction of blood vessels in physiological state, but it can Strongly contract the dilated cerebrovascular and meningeal vessels; By stimulating presynaptic 5-HT1D receptors of the trigeminal nerve, inhibiting the neurogenic inflammatory response and plasma extravasation of the dura mater can reduce the CGRP in the blood during migraine. Calcium gene-related peptide) content; Inhibit the trigeminal nucleus excitation by stimulating the 5-HT1B or 5-HT1D receptors on the brain stem.

(2) The first generation of triptan drugs-sumatriptan:

Before the first triptan drug sumatriptan was marketed in 1992, doctors usually had no good way to treat migraines. They could only take patients with painkillers, ergot alkaloids and diazepam, with an effective rate of about 50%. The ergot alkaloids are very toxic and side effects, and are contraindicated in patients with severe cardiovascular, liver, and kidney diseases; some powerful painkillers may cause terrible rebound in headaches and even lead to drug addiction.

Sumatriptan oral tablets have an effective rate of 60% -80% within 2 hours, whether it is 25mg or 50mg, which is better than the ergotamine + caffeine mixture, and is especially suitable for patients with autonomic symptoms. Some studies have suggested that the effect of oral administration of more than 100mg will not be better, but the incidence of side effects will greatly increase.

Sumatriptan nasal spray 20mg (children 1 ~ 2mg / kg) 15 minutes after the headache can be significantly reduced, after 2 hours, more than 70% of patients can resume normal life and work. Subcutaneous injections work faster, and symptoms such as headaches, blurred vision, and blind spots can be alleviated within 10 minutes. This rapid drug absorption is critical for migraine headaches because the faster the blood plasma concentration is reached and the plasma peak The higher the concentration, the better the overall effect of migraine relief. However, about 40% of patients with a long history of migraine will relapse and need a second injection or other treatment.

(3) The second generation of triptans:

There are currently six second-generation triptans on the market, which have stronger effects and fewer side effects than sumatriptan, and can also relieve the accompanying migraine such as photophobia, phobia, and nausea. symptom. Like antidepressants and antibiotics, different individuals have different sensitivities to different triptans. So more choices means more hope for the patient.

1. Zomitriptan:

Launched in 1996, it has dual effects on both the periphery and the center, and acts on the trigeminal nucleus of the brainstem, which is considered to be the "pain generator" in the brain.

The bioavailability of oral zomitriptan is about 40%, which is higher than that of sumatriptan (14%). Data from a study of 2000 patients showed: 30 minutes after taking 25mg, the effect became effective; 65% to 81% of patients were effective for 2 hours, compared with 15% to 34% of placebo; 47% of patients in the treatment group completely disappeared migraine ; But within 24 hours of administration, the recurrence rate of headache in the treatment group was 21% to 37%.

2. Rizatriptan:

Launched in 1998, it is characterized by: fast onset. The 30-minute medication headache relief rate is 13-28%; The effect is good, the remission rate is 70% after 2 hours of oral administration, and the symptoms disappear after 33%, and the headache is still effective after recurrence; Matriptan 100mg high; side effects are small; wide range of applications, can be used for migraine treatment in patients with hypertension and mild liver dysfunction, can be combined with the antidepressant paroxetine, the treatment of menstrual migraine is still effective.

3 Narathtriptan:

The recommended dosage is 25mg. The peak time of blood medication is 3 to 5 hours after taking the medicine. The average time required for headache relief is about 4 hours.

4 Elitoran:

The effective rate was 84%, and the 24-hour remission rate was higher than other triptans. The incidence of side effects was slightly higher than that of sumatriptan, but they were all mild and there were no serious side effects. Researchers at the New York Headache Institute examined the pharmacokinetics of elitriptan during menstruation and lactation in women. It was found that the menstrual cycle did not significantly change the efficacy of the drug. During breastfeeding, there are very few drugs in the milk, accounting for only 0.02% of the 80mg taken by the mother. Moreover, the nursing mother was very well tolerated with elitriptan, and there were no abnormalities in blood pressure, pulse or electrocardiogram, and no serious side effects occurred. It is also well tolerated by women using contraceptives or hormone replacement therapy.

5. Fluvatriptan (Frotriptan):

Migraine attacks typically last 4-72 hours. Fluvatriptan 2.5 mg tablets reach their maximum concentration in a relatively short time (2-3 hours), with a half-life of 26 hours. This is an important breakthrough when the current half-life of other triptan drugs is less than 6 hours. In addition, there is almost no interaction between the drugs, and the recurrence rate is also low. Long-term patients or patients with a large headache recurrence rate should be considered for use.

6. Amotriptan:

It is the latest and most effective one among triptans. It is characterized by high oral bioavailability (70-80%), rapid onset (75%), and long maintenance time (> 24 hours); recurrence rate Low (24-hour recurrence rate 18-27%); The effect has nothing to do with age, gender, and stomach contents; No cross-reaction with other drugs; The incidence of side effects is extremely low (<1%). Therefore, in the near future, amotriptan is expected to become the first-line drug for migraine.

(IV) Dosage forms of triptans

1. Subcutaneous injection: a fast and effective method for migraine patients. Subcutaneous injection is suitable for patients who have symptoms of nausea, difficulty in oral administration, acute onset, strong pain, and ineffective treatment with other triptans.

2. Intravenous administration: Zomitriptan can be administered by intravenous injection. Intravenous administration of 3.5 mg, mean cmax and auc were 79% and 77%, respectively. Intravenous and oral t1 / 2 were 2.30h and 2.94h, respectively.

3 Oral tablets: Oral tablets are easy to use, patient compliance, tolerability, low cost, but slow action, and patients with nausea are difficult to take. A meta-analysis by Ferrari et al. Showed that within 2 hours, rizatriptan and eritoran had the highest headache response rate; rizatriptan, amotriptan, and elitriptan had the best response to persistent pain-free symptoms; Zaltriptan and amotriptan work quickly; naracetam and amotriptan are best tolerated.

4 Nasal spray: A nasal spray is a fast and effective option for patients who experience nausea and vomiting and who cannot tolerate oral preparations. Compared with subcutaneous administration, it has the advantages of convenient medication and rapid onset of headache relief (as early as 15 minutes), but it has irritation to the nasal cavity, bitterness, improper use, and poor drug absorption. Currently available in this dosage form are sumatriptan and zomitriptan.

5. Orally disintegrating tablets: It is a new dosage form developed in the past ten years, including rizatriptan and zolmitriptan oral disintegrating tablets. Its main feature is that after oral or sublingual administration, it is not necessary to take water. Tablets can disintegrate within 40 seconds under the action of a small amount of saliva, and freeze-dried orally disintegrating tablets can disintegrate within 15 seconds. It is especially suitable for situations where water cannot be taken, such as in the wild, difficulty swallowing, or other situations where rapid administration is required.

6. Rectal suppositories: an alternative route of administration for patients with migraine with significant nausea / vomiting symptoms. Rectal administration avoids some liver first-pass effects, has good curative effect, is well tolerated locally and systemically, and absorbs quickly. Disadvantages are inconvenient medication, patient discomfort, irritation of the rectal mucosa, interruption of drug absorption by defecation, and unstable absorption. Sumatriptan rectal suppositories were approved for sale in September 2002 and are mainly used in Europe.

(5) Problems of side effects:

Tritans generally have lower incidence and severity of side effects than traditional anti-migraine drugs, mainly systemic fever, dry mouth, dizziness, dizziness, discomfort, fatigue, lethargy, paresthesia, and temporary Increasing sexual blood pressure, etc., the incidence rate does not exceed 15%; temporary chest pressure, restraint and chest pain can also be seen (incidence rate 1-4%). Severity may induce coronary spasm or pulmonary hypertension. The best way to avoid serious side effects is to comprehensively assess the patient, master the indications, and take medication as early as possible (to avoid having to increase the dose later).

Patients are generally well tolerated by second-generation triptans, with mild and transient adverse reactions, and often resolve without treatment. Nevertheless, it should be contraindicated in patients with coronary artery disease or any other obvious cardiovascular disease in clinical application, and in patients with uncontrolled hypertension, hemiplegia or basic migraine. There are also reports suggesting that patients with more than two cardiovascular risk factors, those on renal dialysis, or those with moderate liver function impairment should be warned when using triptans.

Amotriptan is the least effective of all triptans. However, for those with severe renal insufficiency, the dose of amotriptan should not exceed 12.5 mg within 24 hours.

(6) Development prospects of triptans:

Since 1999, 4 of the international triptan migraine treatment products have entered the top 500 best-selling prescription drugs in the world, accounting for 95% of the entire migraine treatment market. However, in China, most migraine patients are still at the stage of resting and simply taking painkillers, or have not seen a doctor at all; grassroots doctors use patients with addictive, short-term pain relievers too much, rather than more effective Triptans; China's own development of triptans is limited, and imported drugs are expensive (sumatriptan is about 60 yuan per tablet). These are the issues that need to be solved urgently. It is believed that with the advent of cheaper triptans, increased awareness of grassroots doctors, and increased patient awareness, migraine headaches will no longer be a headache for both patients and doctors.