DIHYDROERGOTAMINE TARTRATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	4C33H37N5O5.C4H6O6
Molecular Weight	2484.7964
Optical Activity	UNSPECIFIED
Defined Stereocenters	30 / 30
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@H]([C@@H](O)C(O)=O)C(O)=O.[H][C@@]12CCCN1C(=O)[C@H](CC3=CC=CC=C3)N4C(=O)[C@](C)(NC(=O)[C@H]5CN(C)[C@]6([H])CC7=CNC8=CC=CC(=C78)[C@@]6([H])C5)O[C@@]24O.[H][C@@]9%10CCCN9C(=O)[C@H](CC%11=CC=CC=C%11)N%12C(=O)[C@](C)(NC(=O)[C@H]%13CN(C)[C@]%14([H])CC%15=CNC%16=CC=CC(=C%15%16)[C@@]%14([H])C%13)O[C@@]%10%12O.[H][C@@]%17%18CCCN%17C(=O)[C@H](CC%19=CC=CC=C%19)N%20C(=O)[C@](C)(NC(=O)[C@H]%21CN(C)[C@]%22([H])CC%23=CNC%24=CC=CC(=C%23%24)[C@@]%22([H])C%21)O[C@@]%18%20O.[H][C@@]%25%26CCCN%25C(=O)[C@H](CC%27=CC=CC=C%27)N%28C(=O)[C@](C)(NC(=O)[C@H]%29CN(C)[C@]%30([H])CC%31=CNC%32=CC=CC(=C%31%32)[C@@]%30([H])C%29)O[C@@]%26%28O

InChI

InChIKey=FXDJFTCVYTUARH-YZPGULDNSA-N

InChI=1S/4C33H37N5O5.C4H6O6/c4*1-32(35-29(39)21-15-23-22-10-6-11-24-28(22)20(17-34-24)16-25(23)36(2)18-21)31(41)38-26(14-19-8-4-3-5-9-19)30(40)37-13-7-12-27(37)33(38,42)43-32;5-1(3(7)8)2(6)4(9)10/h4*3-6,8-11,17,21,23,25-27,34,42H,7,12-16,18H2,1-2H3,(H,35,39);1-2,5-6H,(H,7,8)(H,9,10)/t4*21-,23-,25-,26+,27+,32-,33+;1-,2-/m11111/s1

HIDE SMILES / InChI

Molecular Formula	C33H37N5O5
Molecular Weight	583.6774
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	C4H6O6
Molecular Weight	150.0868
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12558771 | https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf

Dihydroergotamine (DHE) is a semisynthetic, hydrogenated ergot alkaloid, synthesized by reducing an unsaturated bond in ergotamine. Dihydroergotamine was originally envisaged as an antihypertensive agent, but it was later shown to be highly effective in treating migraine. Dihydroergotamine was first used to treat migraine in 1945 by Horton, Peters, and Blumenthal at the Mayo Clinic. In 1986, Raskin and Callaham reconfirmed the effectiveness of DHE for both intermittent and intractable migraine. The use of DHE was reviewed by Scott in 1992. In 1997, a nasal spray version was approved for use in migraine. Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Dihydroergotamine binds with high affinity to 5-HT1Dα and 5-HT1Dβ receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline α2A, α2B and α, receptors, and dopamine D2L and D3 receptors. The therapeutic activity of dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. Two current theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine. One theory suggests that activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache. The alternative hypothesis suggests that activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of proinflammatory neuropeptide release.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Serotonin 1d (5-HT1d) receptor 52 Target ID: CHEMBL1983 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/9605573 \| https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	0.5 nM [IC50]
Serotonin 1b (5-HT1b) receptor 45 Target ID: CHEMBL1898 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/9605573 \| https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	0.7 nM [IC50]
Serotonin 1a (5-HT1a) receptor 171 Target ID: CHEMBL214 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	0.4 nM [IC50]
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL224 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	9.0 nM [IC50]
Serotonin 2c (5-HT2c) receptor 122 Target ID: CHEMBL225 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	1.3 nM [IC50]
Serotonin 1f (5-HT1f) receptor 15 Target ID: CHEMBL1805 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12558771	Agonist 2662	180.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Migraine 103 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	Primary		Approved 8360	D.H.E. 45 Approved Use Dihydroergotamine Mesylate Injection, USP is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Launch Date -7.48656E11

C_max

Value	Dose	Co-administered	Analyte	Population
1.02 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8841149/	1 mg single, nasal dose: 1 mg route of administration: Nasal experiment type: SINGLE co-administered:		DIHYDROERGOTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
5.05 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8841149/	1 mg single, nasal dose: 1 mg route of administration: Nasal experiment type: SINGLE co-administered:		DIHYDROERGOTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.952 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8841149/	1 mg single, nasal dose: 1 mg route of administration: Nasal experiment type: SINGLE co-administered:		DIHYDROERGOTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
7% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8841149/	1 mg single, nasal dose: 1 mg route of administration: Nasal experiment type: SINGLE co-administered:		DIHYDROERGOTAMINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	Disc. AE: Rhinitis, Dizziness... AEs leading to discontinuation/dose reduction: Rhinitis (2 patients) Dizziness (2 patients) Edema face (1 patient) Cold sweat (1 patient) Trauma (1 patient) Depression (1 patient) Somnolence (1 patient) Allergy (1 patient) Vomiting (1 patient) Hypotension (1 patient) Paraesthesia (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
4 mg 1 times / day steady, intranasal Highest studied dose Dose: 4 mg, 1 times / day Route: intranasal Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf
1 mg single, subcutaneous Recommended Dose: 1 mg Route: subcutaneous Route: single Dose: 1 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	Disc. AE: Cerebrovascular event... AEs leading to discontinuation/dose reduction: Cerebrovascular event (grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf
1 mg 1 times / day steady, subcutaneous (max) Recommended Dose: 1 mg, 1 times / day Route: subcutaneous Route: steady Dose: 1 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/	unhealthy, adult n = 51 Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Population Size: 51 Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/	Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (20 patients) Vomiting (3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/

AEs

AE	Significance	Dose	Population
Allergy	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Cold sweat	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Depression	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Edema face	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Hypotension	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Paraesthesia	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Somnolence	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Trauma	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Vomiting	1 patient Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Dizziness	2 patients Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Rhinitis	2 patients Disc. AE	2 mg single, intranasal Studied dose Dose: 2 mg Route: intranasal Route: single Dose: 2 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf	unhealthy, 18 - 65 years n = 1796 Health Status: unhealthy Condition: migraine Age Group: 18 - 65 years Sex: M+F Population Size: 1796 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020148Orig1s025lbl.pdf
Cerebrovascular event	grade 5 Disc. AE	1 mg single, subcutaneous Recommended Dose: 1 mg Route: subcutaneous Route: single Dose: 1 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20148s7s8lbl.pdf
Nausea	20 patients Disc. AE	1 mg 1 times / day steady, subcutaneous (max) Recommended Dose: 1 mg, 1 times / day Route: subcutaneous Route: steady Dose: 1 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/	unhealthy, adult n = 51 Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Population Size: 51 Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/
Vomiting	3 patients Disc. AE	1 mg 1 times / day steady, subcutaneous (max) Recommended Dose: 1 mg, 1 times / day Route: subcutaneous Route: steady Dose: 1 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/	unhealthy, adult n = 51 Health Status: unhealthy Condition: migraine Age Group: adult Sex: unknown Population Size: 51 Sources: https://pubmed.ncbi.nlm.nih.gov/8984085/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1437 MATE1 304 MATE2 261 OCT2 638

Drug as perpetrator

Target	Modality	Activity
MATE2 261	inhibitor 3240 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068829/	yes [IC50 12.6 uM]
MATE1 306	inhibitor 3240 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068829/	yes [IC50 2.8 uM]
OCT2 639	inhibitor 3240 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068829/	yes [IC50 49.9 uM]
P-gp 1626	inhibitor 3240 Sources: https://jpet.aspetjournals.org/content/303/1/323.long Page: 5.0	yes [Ki 120 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1709	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC152687/	yes

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:4562	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4562
ZINC	ZINC000003978005	http://zinc15.docking.org/substances/ZINC000003978005

PubMed

Title	Date	PubMed
Clinical ergotism induced by ritonavir.	2001	11728055
Sumatriptan by injection.	2001	11678812
When should triptans be taken during a migraine attack?	2001	11524030
[Migraine: selection of therapeutic agents to be applied during its attack].	2001 Apr 10	11391906
Current concepts of pelvic congestion and chronic pelvic pain.	2001 Apr-Jun	11394421
Treatment and management of cluster headache.	2001 Feb	11252143
Ergot alkaloid transport across ruminant gastric tissues.	2001 Feb	11219466
[Therapy and prevention of migraine. New recommendations and their practical application].	2001 Feb 22	11265538
[Ormond's fibrosis, bone osteolysis and stomach intramural metastases in the course f low-differentiated prostatic cancer].	2001 Jul	11928571
Complicated migraine and migraine variants.	2001 Mar	11332867
Effect of an acute ergotamine challenge on reproductive hormones in follicular phase heifers and progestin-treated cows.	2001 May 31	11348777
In vitro effect of alkaloids on bloodstream forms of Trypanosoma brucei and T. congolense.	2001 Oct	11582539
[Migraine and facial pain].	2001 Oct 15	11795132
A simple thin-layer chromatographic method for the detection of ergovaline in leaf sheaths of tall fescue (Festuca arundinacea) infected with Neotyphodium coenophialum.	2001 Sep	11580073
Efficacy, tolerability and safety of oral eletriptan and ergotamine plus caffeine (Cafergot) in the acute treatment of migraine: a multicentre, randomised, double-blind, placebo-controlled comparison.	2002	11844898
Frovatriptan: a review of drug-drug interactions.	2002 Apr	12028322
Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization.	2002 Apr	11888550
Therapeutic strategies for orthostatic intolerance: mechanisms, observations, and making patients feel better.	2002 Apr 1	11904120
Management of the acute migraine headache.	2002 Dec 1	12484694
Possible ergotamine-caffeine-associated delirium.	2002 Jan	11794425
Endocardial myxomatous change in Harlan Sprague-Dawley rats (Hsd:S-D) and CD-1 mice: its microscopic resemblance to drug-induced valvulopathy in humans.	2002 Jul-Aug	12187939
Endocrine and respiratory responses to ergotamine in Brahman and Hereford steers.	2002 Jun	12046966
New treatments in cluster headache.	2002 Mar	11898477
Treatment patterns of isolated benign headache in US emergency departments.	2002 Mar	11867972
Sensitive and specific liquid chromatographic-tandem mass spectrometric assay for dihydroergotamine and its major metabolite in human plasma.	2002 Mar 5	11888055
Incidence and determinants of migraine prophylactic medication in the Netherlands.	2002 May	12012149
Buccal absorption of ergotamine tartrate using the bioadhesive tablet system in guinea-pigs.	2002 May 15	11996820
Pharmacological characterization of 5-HT(1B) receptor-mediated inhibition of local excitatory synaptic transmission in the CA1 region of rat hippocampus.	2003 Jan	12522075
Variations among emergency departments in the treatment of benign headache.	2003 Jan	12514688

Patents

Sample Use Guides

In Vivo Use Guide

Usual Adult Dose for Migraine IM or subcutaneous: Initial dose: 1 mg given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given hourly until the headache has stopped or a total dose of 3 mg has been reached. The total weekly dose should not exceed 6 mg. IV: Initial dose: 1 mg given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given hourly until the headache has stopped or a total dose of 2 mg has been reached. The total weekly dose should not exceed 6 mg. Intranasal: 1 spray (0.5 mg) into each nostril (total = 1 mg). Repeat if needed within 15 minutes to a maximum of 4 sprays (2 mg) per day. The total weekly dose should not exceed 8 sprays (4 mg). Usual Adult Dose for Cluster Headache IM or subcutaneous: Initial dose: 1 mg given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given hourly until the headache has stopped or a total dose of 3 mg has been reached. The total weekly dose should not exceed 6 mg. IV: Initial dose: 1 mg given as quickly as possible after the first symptom of headache. Additional 1 mg doses can be given hourly until the headache has stopped or a total dose of 2 mg has been reached. The total weekly dose should not exceed 6 mg.

Route of Administration: Other

In Vitro Use Guide

Dihydroergotamine (DHE) (EC(50)=10.9+/-0.3 nM) and 8'-OH-DHE (EC(50)=30.4+/-0.8 nM) inhibited the firing of serotoninergic neurons in the rat dorsal raphe nucleus within brain stem slices.

Substance Class	Chemical Created by `admin` on `Thu Jul 06 01:49:41 UTC 2023` Edited by `admin` on `Thu Jul 06 01:49:41 UTC 2023`
Record UNII	76F2R89O7X
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DIHYDROERGOTAMINE TARTRATE

Common Name

English

Dihydroergotamine tartrate [WHO-DD]

Common Name

English

Code System Code Type Description

FDA UNII

76F2R89O7X