Drug Reference for FDA Approved Parkinson's Disease Drugs

Drug Reference for FDA Approved Migraine Drugs @ Neurotransmitter.net

Only the most well known trade name is listed for each drug. Some dosage forms/routes may be sold under different trade names. Use the FDA link to find out about the trade names under which the various dosage forms are sold.
Some of the major metabolites listed are not active metabolites.
Off-label indications are not included.
MDL Chime is required to view the "3D" chemical structures.
The possible mechanisms of action that I have suggested should be subjected to critical inquiry. Please consult PubMed, the PDSP K_i database, and the referenced literature to decide for yourself if my descriptions are accurate.
Drug references for FDA approved psychiatric drugs, FDA approved general anesthetic drugs, FDA approved opioid painkillers, FDA approved epilepsy drugs, FDA approved Alzheimer's disease drugs, FDA approved Parkinson's disease drugs, and FDA approved muscle relaxants and related drugs are also available.
E-mail Shawn Thomas if you have any suggestions about how this resource could be improved.
This page has been sponsored by Epocrates, Inc.
Updated 9/23/05

Generic Name:
acetaminophen, aspirin, and caffeine

Trade Name:
Excedrin Migraine ® [Bristol-Myers Squibb]

Dosage Forms/Routes:
tablet/oral

Major Metabolites:
Acetaminophen:
acetaminophen glucuronide; acetaminophen sulfate
Aspirin:
salicylic acid;
gentisic acid;
salicyluric acid
Caffeine:
paraxanthine;
theophylline;
theobromine

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]

Initial Approval:
01/14/1998

Manufacturers:
[FDA Search]

Product Label :
[Link]

Indications:
Excedrin Migraine is indicated for the treatment of migraine.

Possible Mechanisms of Action:
Acetaminophen inhibits cyclooxygenase-2 (COX-2) when concentrations of arachidonic acid and peroxides are low (1). In addition, acetaminophen inhibits the apozyme of tryptophan-2,3-dioxygenase in the liver (2).

Aspirin (acetylsalicylic acid) acetylates vascular COX-2, which causes it to catalyze the synthesis of aspirin-triggered 15-epi-lipoxin intermediates rather than the synthesis of prostaglandin intermediates (3). Aspirin is also an irreversible inhibitor of cyclooxygenase-1 (COX-1) (4).

Caffeine is a competitive antagonist at A1 and A2A adenosine receptors (5). The drug is also a nonselective phosphodiesterase inhibitor; however, normal consumption of caffeine is not likely to induce this effect (6).

Chemical Classes:
acetanilide derivative (acetaminophen), salicylic acid derivative (aspirin), and methylxanthine (caffeine)
"3D" Structure (Requires Chime):
[Link (acetaminophen)]
[Link (aspirin)]
[Link (caffeine)]

Generic Name:
almotriptan malate

Trade Name:
Axert ® [Ortho-McNeil]

IUPAC Name:
N,N-dimethyl-2-[5-(pyrrolidin-
1-ylsulfonylmethyl)-1H-indol-
3-yl]-ethanamine; 2-
hydroxybutanedioic acid

Dosage Forms/Routes:
Tablet/oral

Major Metabolites:
M2 (formed by pyrrolidine ring oxidation);
M6 (indole acetic acid derivative);
M8 (glucuronide acid metabolite of M6) (see McEwen et al., 2004)

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
05/07/2001

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₂₁H₃₁N₃O₇S

Molecular Mass:
469.553 g/mol

Indications:
Almotriptan tablets are indicated for the acute treatment of migraine with or without aura in adults.

Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS in the prescribing information). Safety and effectiveness of almotriptan have not been established for cluster headache, which is present in an older, predominantly male population.

Possible Mechanisms of Action:
Almotriptan is an agonist at serotonin 5-HT1B, 5-HT1D, and 5-HT1F receptors (7).

Chemical Class:
triptan

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
aspirin

Trade Name:
Aspirin Migraine ® [Bayer]

IUPAC Name:
2-acetyloxybenzoic acid

Dosage Forms/Routes:
tablet/oral

Major Metabolites:
salicylic acid;
gentisic acid;
salicyluric acid

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
10/18/2001

Manufacturers:
[FDA Search]

Product Label :
[Link]

Epocrates:
[Link]

Empirical Formula:
C₉H₈O₄

Molecular Mass:
180.157 g/mol

Indications:
Excedrin Migraine is indicated for the treatment of migraine.

Possible Mechanisms of Action:
Aspirin (acetylsalicylic acid) acetylates vascular COX-2, which causes it to catalyze the synthesis of aspirin-triggered 15-epi-lipoxin intermediates rather than the synthesis of prostaglandin intermediates (3). Aspirin is also an irreversible inhibitor of cyclooxygenase-1 (COX-1) (4).

Chemical Classes:
salicylic acid derivative

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
caffeine and ergotamine tartrate

Trade Name:
Cafergot ® [Novartis]

IUPAC Name (caffeine) :
1,3,7-trimethylpurine-2,6-dione

Common Chemical Name (ergotamine tartrate):
Ergotaman-3',6', 18-trione,
12'- hydroxy-2'-methyl-5'-
(phenyl-methyl)-,(5'(alpha))-,
[R-(R*,R*)]-2, 3-dihydroxybutanedioate(2:1)
(tartrate)

Dosage Forms/Routes:
Tablet/oral;
Suppository/rectal

Major Metabolites:
Caffeine:
paraxanthine;
theophylline;
theobromine
Ergotamine:
M1; M2; M1-Iso; M2-Iso (see Moubarak and Rosenkrans Jr., 2000)

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]

Initial Approval:
11/26/1948

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₄₅H₅₁N₉O₁₂

Molecular Mass:
909.94 g/mol

Indications:
The combination of caffeine and ergotamine is indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so-called "histaminic cephalalgia."

Possible Mechanisms of Action:
Caffeine is a competitive antagonist at A1 and A2A adenosine receptors (5). The drug is also a nonselective phosphodiesterase inhibitor; however, normal consumption of caffeine is not likely to induce this effect (6).

Ergotamine is an agonist at serotonin 5-HT1A (8), 5-HT1B (8), 5-HT1D (8), 5-HT2A (9), 5-HT2B (9), 5-HT2C (9), 5-HT5A (10), and 5-HT6 (11) receptors. Ergotamine also binds relatively weakly to serotonin 5-HT1F receptors (12), alpha-2A-adrenoceptors (13), and alpha-2B-adrenoceptors (13). In addition, ergotamine may accelerate the transport of glutamate mediated by hGluT-1 (19).

Chemical Class:
methylxanthine (caffeine) and ergot alkaloid (ergotamine)

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link (caffeine)]
[Link (ergotamine)]

Generic Name:
dihydroergotamine mesylate

Trade Name:
D.H.E. 45 ® [Valeant]

Common Chemical Name:
ergotaman-3',6',18-
trione,9,10-dihydro-12'-
hydroxy-2'-methyl-5'-
(phenylmethyl) (5'a)-, monomethanesulfonate

Dosage Forms/Routes:
Injectable/injection;
Spray, metered/nasal

Major Metabolite:
8'-hydroxy-dihydroergotamine

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
04/12/1946

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₃₄H₄₁N₅O₈S

Molecular Mass:
679.784 g/mol

Indications:
Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes.

Possible Mechanisms of Action:
Dihydroergotamine is an agonist at serotonin 5-HT1A (14), 5-HT1B (14), 5-HT1D (14), 5-HT1F (15), 5-HT2B (16), and 5-HT2C (16) receptors. The drug is an antagonist at serotonin 5-HT2A receptors (17). Dihydroergotamine may also bind to alpha-1-adrenoceptors, alpha-2-adrenoceptors, and dopamine D2 receptors (18). In addition, dihydroergotamine may accelerate the transport of glutamate mediated by hGluT-1 (19).

Chemical Class:
semisynthetic, hydrogenated ergot alkaloid

PubChem 2D Structure:

Generic Name:
divalproex sodium

Trade Name:
Depakote ® [Abbott Labs]

IUPAC Name:
sodium; 2-propylpentanoate;
2-propylpentanoic acid

Major Metabolites:
3-keto-valproic acid;
trans-2-ene valproic acid;
valproic acid glucuronide

Dosage Forms/Routes:
Tablet (delayed release)/oral;
Capsule (delayed release pellets)/oral;
Tablet (extended release)/oral

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
03/10/1983

Manufacturers:
[FDA Search]

Prescribing Information:
[Link 1]
[Link 2] (ER)

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₁₆H₃₁NaO₄

Molecular Mass:
310.405 g/mol

Indications:
Prophylaxis of migraine headaches; monotherapy and adjunctive therapy in the treatment of patients with complex partial seizures that occur either in isolation or in association with other types of seizures; sole or adjunctive therapy in the treatment of simple and complex absence seizures; adjunct for the treatment of patients with multiple seizure types that include absence seizures; manic episodes associated with bipolar disorder

Possible Mechanisms of Action:
Divalproex is a histone deacetylase inhibitor (20). The enhancement of gamma-aminobutyric acid (GABA) activity by divalproex is possibly due to the downregulation of GAT-1 and GAT-3 GABA transporter proteins by the drug (21); the cause of this effect is currently unknown. Divalproex also inhibits succinate semialdehyde dehydrogenase (22). At voltage-gated sodium channnels, divalproex shifts the voltage dependence of steady-state inactivation to more hyperpolarized potentials (23); the degree to which this action occurs at therapeutically relevant concentrations in humans is currently not known (24). Finally, divalproex may inhibit T-type calcium channels (25).

Chemical Class:
carboxylic acid derivative

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
eletriptan hydrobromide

Trade Name:
Relpax ® [Pfizer]

IUPAC Name:
3-[(1-methylpyrrolidin-2-yl)
methyl]-5-(2-
phenylsulfonylethyl)-1H-indole
hydrobromide

Dosage Forms/Routes:
Tablet/oral

Major Metabolite:
N-desmethyl eletriptan

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
12/26/2002

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₂₂H₂₇BrN₂O₂S

Molecular Mass:
463.432 g/mol

Indications:
Eletriptan tablets are indicated for the acute treatment of migraine with or without aura in adults.

Eletriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS in the prescribing information). Safety and effectiveness of eletriptan have not been established for cluster headache, which is present in an older, predominantly male population.

Possible Mechanisms of Action:
Eletriptan is an agonist at serotonin 5-HT1B, 5-HT1D, and 5-HT1F receptors (26).

Chemical Class:
triptan

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
ergotamine tartrate

Trade Name:
Ergomar ® [Harvest]

Common Chemical Name:
Ergotaman-3',6', 18-trione,
12'-hydroxy-2'-methyl-5'-
(phenyl-methyl)-,(5'(alpha))-
,[R-(R*,R*)]-2, 3-
dihydroxybutanedioate(2:1)
(tartrate)

Dosage Forms/Routes:
Tablet/sublingual

Major Metabolites:
M1; M2; M1-Iso; M2-Iso (see Moubarak and Rosenkrans Jr., 2000)

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
02/24/1983

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Empirical Formula:
C₃₇H₄₁N₅O₁₁

Molecular Mass:
731.749 g/mol

Indications:
Ergotamine is indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so-called "histaminic cephalalgia."

Possible Mechanisms of Action:
Ergotamine is an agonist at serotonin 5-HT1A (8), 5-HT1B (8), 5-HT1D (8), 5-HT2A (9), 5-HT2B (9), 5-HT2C (9), 5-HT5A (10), and 5-HT6 (11) receptors. Ergotamine also binds relatively weakly to serotonin 5-HT1F receptors (12), alpha-2A-adrenoceptors (13), and alpha-2B-adrenoceptors (13). In addition, ergotamine may accelerate the transport of glutamate mediated by hGluT-1 (19).

Chemical Class:
ergot alkaloid

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
frovatriptan succinate

Trade Name:
Frova ® [Endo]

IUPAC Name:
butanedioic acid; 6-
methylamino-6,7,8,9-
tetrahydro-5H-carbazole-3-
carboxamide; hydrate

Dosage Forms/Routes:
Tablet/oral

Major Metabolites:
hydroxylated frovatriptan;
N-acetyl desmethyl frovatriptan; hydroxylated N-acetyl desmethyl frovatriptan;
desmethyl frovatriptan

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
11/08/2001

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₁₈H₂₅N₃O₆

Molecular Mass:
379.408 g/mol

Indications:
Frovatriptan tablets are indicated for the acute treatment of migraine with or without aura in adults.

Frovatriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see CONTRAINDICATIONS in the prescribing information). Safety and effectiveness of frovatriptan have not been established for cluster headache, which is present in an older, predominantly male population.

Possible Mechanisms of Action:
Frovatriptan is an agonist at 5-HT1B (27), 5-HT1D (27), and 5-HT1F (28) receptors. At higher concentrations, the drug is an agonist at 5-HT7 receptors (27, 29).

Chemical Class:
triptan

PubChem 2D Structure:

Generic Name:
ibuprofen

Trade Name:
Motrin Migraine Pain ® [McNeil]

IUPAC Name:
2-[4-(2-
methylpropyl)phenyl]propanoic acid

Dosage Forms/Routes:
Tablet/oral

Major Metabolites:
(+)-2-4'-(2-hydroxy-2-
methylpropyl)-phenylpropionic acid;
(+)-2-4'-(2-carboxypropyl)-
phenylpropionic acid

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
05/18/1984

Manufacturers:
[FDA Search]

Product Label :
[Link]

Epocrates:
[Link]

Empirical Formula:
C₁₃H₁₈O₂

Molecular Mass:
206.281 g/mol

Indications:
Motrin Migraine Pain is indicated for the treatment of migraine.

Possible Mechanisms of Action:
Ibuprofen inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) (45). It is a less potent inhibitor of the latter enzyme (45).

Chemical Class:
propionic acid derivative

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
ibuprofen potassium

Trade Name:
Advil Migraine ® [Wyeth]

IUPAC Name:
potassium 2-[4-(2-
methylpropyl)phenyl]propanoate

Dosage Forms/Routes:
Capsule/oral

Major Metabolites:
(+)-2-4'-(2-hydroxy-2-
methylpropyl)-phenylpropionic acid;
(+)-2-4'-(2-carboxypropyl)-
phenylpropionic acid

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
04/20/1995

Manufacturers:
[FDA Search]

Product Label:
[Link]

Epocrates:
[Link]

Empirical Formula:
C₁₃H₁₇KO₂

Molecular Mass:
244.371 g/mol

Indications:
Advil Migraine is indicated for the treatment of migraine.

Possible Mechanisms of Action:
Ibuprofen inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) (45). It is a less potent inhibitor of the latter enzyme (45).

Chemical Class:
propionic acid derivative

PubChem 2D Structure:

"3D" Structure (Requires Chime):
[Link]

Generic Name:
naratriptan hydrochloride

Trade Name:
Amerge ® [GlaxoSmithKline]

IUPAC Name:
N-methyl-2-[3-(1-methyl-4-
piperidyl)-1H-indol-5-yl]-
ethanesulfonamide hydrochloride

Dosage Forms/Routes:
Tablet/oral

Major Metabolite:
N-oxide of naratriptan

Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP K_i database]

Initial Approval:
02/10/1998

Manufacturers:
[FDA Search]

Prescribing Information:
[Link]

RxList:
[Link]

Epocrates:
[