II. Mechanism
- Identical mechanism as with Guanethidine, but with faster activity, and shorter Half-Life
- Transiently increases Norepinephrine release from nerve terminals (with transient Hypertension and Tachycardia)
- Subsequent decreased Norepinephrine release via depletion of Norepinephrine from nerve stores
- Prevents Norepinephrine release at nerve endings
- Poorly crosses blood brain barrier
- No sedation (contrast with Reserpine)
III. Pharmacokinetics
- Incompletely absorbed orally (similar to Guanethidine)
- Half is Metabolized
-
Half-Life: 12 hours
- Contrast with the very long, 5 day half life of Guanethidine
IV. Indications
- Rarely used in United States
- May have a place in Hypertension, but has been replaced by newer agents with fewer adverse effects
V. Contraindications
VI. Adverse Effects
- Effects are less severe than with Guanethidine
- Transient Hypertension and Tachycardia (see mechanism above)
-
Hypotension
- Reflex Tachycardia mechanism blocked by loss of Norepinephrine release
- Decreased Cardiac Output
- Bradycardia
- COPD Exacerbation
- Nasal congestion (significantly increased)
VII. Drug Interactions
-
Tricyclic Antidepressants (TCA)
- TCAs block Guanethidine entry into cells
VIII. References
- Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 64-5
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Related Studies
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C004945 |
| SnomedCT | 372820001, 69204002 |
| English | (1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine, guanadrel, guanadrel [Chemical/Ingredient], Guanadrel, Guanadrel (product), Guanadrel (substance), GUANADREL |
| Spanish | guanadrel (producto), guanadrel (sustancia), guanadrel |
Ontology: Hylorel (C0720982)
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C004945 |
| English | Hylorel, Celltech brand of guanadrel sulfate |
