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US Approved Rx

3

Other

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Primary Target

Serotonin 1a (5-HT1a) receptor

2

Serotonin 1b (5-HT1b) receptor

2

Serotonin 1d (5-HT1d) receptor

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Serotonin 1f (5-HT1f) receptor

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Cyclooxygenase-1

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1992

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1991

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Cluster headache

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Migraine with aura

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Osteoarthritis

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Rheumatoid arthritis

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Glaxo

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ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS

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ATC Level 4

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SUMATRIPTAN

8R78F6L9VO

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Status:

US Approved Rx (2021)

First approved in 1992

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Serotonin 1d (5-HT1d) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1f (5-HT1f) receptor

Serotonin 1a (5-HT1a) receptor

Conditions:

Cluster headache

Migraine without aura

Migraine with aura

Sumatriptan is a serotonin (5-HT1B/1D) receptor agonist indicated for acute treatment of migraine with or without aura in adults. Sumatriptan is structurally similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT1D and 5-HT1B) agonist. The ...

specific receptor subtypes it activates are present on the cranial arteries and veins. Acting as an agonist at these receptors, sumatriptan reduces the vascular inflammation associated with migraines. The specific receptor subtype it activates is present in the cranial and basilar arteries. Activation of these receptors causes vasoconstriction of those dilated arteries. Sumatriptan is also shown to decrease the activity of the trigeminal nerve, which presumably accounts for sumatriptan's efficacy in treating cluster headaches. The injectable form of the drug has been shown to abort a cluster headache within 30 minutes in 77% of cases. Sumatriptan is effective for ending or relieving the intensity of migraine and cluster headaches. It is most effective taken early after the start of the pain. Injected sumatriptan is more effective than other formulations. Large doses of sumatriptan can cause sulfhemoglobinemia, a rare condition in which the blood changes from red to greenish-black, due to the integration of sulfur into the hemoglobin molecule. Serious cardiac events, including some that have been fatal, have occurred following the use of sumatriptan injection or tablets. Events reported have included coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation (V-Fib).

NABUMETONE

LW0TIW155Z

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Status:

US Approved Rx (2011)

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Cyclooxygenase-2

Cyclooxygenase-1

Conditions:

Rheumatoid arthritis

Nabumetone is a naphthylalkanone. Is is a non-selective prostaglandin G/H synthase (a.k.a. cyclooxygenase or COX) inhibitor that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of ar...

achidonic acid to prostaglandin G2 and prostaglandin G2 to prostaglandin H2. Prostaglandin H2 is the precursor to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. The parent compound is a prodrug that undergoes hepatic biotransformation to the active compound, 6-methoxy-2-naphthylacetic acid (6MNA). The analgesic, antipyretic and anti-inflammatory effects of NSAIDs occur as a result of decreased prostaglandin synthesis. The parent compound is a prodrug, which undergoes hepatic biotransformation to the active component, 6-methoxy-2-naphthylacetic acid (6MNA), that is a potent inhibitor of prostaglandin synthesis, most likely through binding to the COX-2 and COX-1 receptors. Nabumetone is used for acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis. Nabumetone has been developed by Beecham. It is available under numerous brand names, such as Relafen, Relifex, and Gambaran.

ZOLMITRIPTAN, (R)-

F3YOE57701

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

SUMATRIPTAN SUCCINATE

J8BDZ68989

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Status:

US Approved Rx (2021)

First approved in 1992

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Serotonin 1d (5-HT1d) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1f (5-HT1f) receptor

Serotonin 1a (5-HT1a) receptor

Conditions:

Cluster headache

Migraine without aura

Migraine with aura

Sumatriptan is a serotonin (5-HT1B/1D) receptor agonist indicated for acute treatment of migraine with or without aura in adults. Sumatriptan is structurally similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT1D and 5-HT1B) agonist. The ...

specific receptor subtypes it activates are present on the cranial arteries and veins. Acting as an agonist at these receptors, sumatriptan reduces the vascular inflammation associated with migraines. The specific receptor subtype it activates is present in the cranial and basilar arteries. Activation of these receptors causes vasoconstriction of those dilated arteries. Sumatriptan is also shown to decrease the activity of the trigeminal nerve, which presumably accounts for sumatriptan's efficacy in treating cluster headaches. The injectable form of the drug has been shown to abort a cluster headache within 30 minutes in 77% of cases. Sumatriptan is effective for ending or relieving the intensity of migraine and cluster headaches. It is most effective taken early after the start of the pain. Injected sumatriptan is more effective than other formulations. Large doses of sumatriptan can cause sulfhemoglobinemia, a rare condition in which the blood changes from red to greenish-black, due to the integration of sulfur into the hemoglobin molecule. Serious cardiac events, including some that have been fatal, have occurred following the use of sumatriptan injection or tablets. Events reported have included coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia, and ventricular fibrillation (V-Fib).

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