Guanethidine
CARDIOVASCULAR SYSTEM
Also known as: abapresin, guanethidine monosulfate, guanethidine sulfate, ismelin, octatensine, oktatensin
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Guanethidine is an ofm drug catalogued in DrugCentral. It was first approved by the FDA in 1960. DrugCentral lists 7 molecular targets, including ADRA2A, SLC6A2 and ADRA1A. Recorded indications include Hypertensive disorder.
- Approval status: ofm (first approved 1960 by the FDA).
- Molecular targets: ADRA2A, SLC6A2, ADRA1A and ADRA2B (7 listed in DrugCentral).
- Indications: Hypertensive disorder.
- ATC code: C02CC02 (Guanidine derivatives).
- Molecular formula: C10H22N4; molecular weight 198.31 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (1)
- Hypertensive disorder
Contraindications (20)
- Acute pancreatitis
- Anuria
- Azotemia
- Dehydration
- Diabetes mellitus
- Gout
- Hepatic coma
- Hypercalcemia
- Hypercholesterolemia
- Hyperparathyroidism
- Hyperuricemia
- Hypochloremic alkalosis
- Hypokalemia
- Hypomagnesemia
- Hyponatremia
- Hypovolemia
- Neonatal hyperbilirubinemia
- Secondary angle-closure glaucoma
- Sympathectomy
- Systemic lupus erythematosus
Mechanism & targets
Molecular targets (7)
| Target | Gene | Action | Activity |
|---|---|---|---|
| Alpha-2A adrenergic receptor | ADRA2A | unknown | — |
| Sodium-dependent noradrenaline transporter | SLC6A2 | substrate | — |
| Alpha-1A adrenergic receptor | ADRA1A | unknown | — |
| Alpha-2B adrenergic receptor | ADRA2B | unknown | — |
| Alpha-2C adrenergic receptor | ADRA2C | unknown | — |
| Alpha-1D adrenergic receptor | ADRA1D | unknown | — |
| Alpha-1B adrenergic receptor | ADRA1B | unknown | — |
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 1960-07-05 | FDA | — | — |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
C02CC02 | CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING › Guanidine derivatives |
C02LF01 | CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION › Guanidine derivatives and diuretics |
S01EX01 | SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Other antiglaucoma preparations |
Chemical structure
Full physicochemical, ADMET and 3D-structure analysis of Guanethidine is on its molecule page.
| Molecular formula | C10H22N4 |
|---|---|
| Molecular weight | 198.31 g/mol |
| CAS number | 55-65-2 |
| InChIKey | ACGDKVXYNVEAGU-UHFFFAOYSA-N |
| PubChem CID | 3518 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Guanethidine used for?
DrugCentral lists the following indications for Guanethidine: Hypertensive disorder.
How does Guanethidine work?
Its molecular targets in DrugCentral include ADRA2A, SLC6A2 (substrate), ADRA1A and ADRA2B.
When was Guanethidine first approved?
Guanethidine was first approved by the FDA in 1960.
What is the chemical formula of Guanethidine?
Guanethidine has the molecular formula C10H22N4 and a molecular weight of 198.31 g/mol.
Browse: all drugs starting with G · drug guides by category · protein targets A–Z.
Sources
- DrugCentral drug card 1342 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL1345 — compound record and bioactivity
- PubChem CID 3518 — chemical identifiers
- DrugBank DB01170 — drug record
- FDA UNII ZTI6C33Q2Q — substance identity
- DailyMed: FDA labels for Guanethidine — current prescribing information (label search)
- UniProt P08913 (ADRA2A) — target protein
- UniProt P23975 (SLC6A2) — target protein
- UniProt P35348 (ADRA1A) — target protein
- UniProt P18089 (ADRA2B) — target protein
- UniProt P18825 (ADRA2C) — target protein
- UniProt P25100 (ADRA1D) — target protein
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