Guanethidine is a peripheral adrenergic neuron-blocking agent that was historically used as an antihypertensive drug. It reduces sympathetic nervous system activity by interfering with the storage and release of norepinephrine from peripheral sympathetic nerve terminals.
Guanethidine is commonly encountered in pharmaceutical use as guanethidine monosulfate.
Guanethidine is a specialized cardiovascular pharmaceutical active ingredient. Its manufacture involves controlled chemical synthesis, purification and analytical testing to ensure consistent identity, purity, assay and impurity profile.
CAS Number: 55-65-2
Molecular Formula: C10H22N4O2
Molecular Weight: 230.31 g/mol
Common Pharmaceutical Form: Guanethidine Monosulfate
Drug Class: Adrenergic Neuron Blocking Agent
Therapeutic Class: Antihypertensive
Therapeutic Area: Cardiovascular
Guanethidine is transported into peripheral sympathetic nerve terminals through the norepinephrine transporter (NET). It becomes concentrated in storage vesicles and interferes with the release of norepinephrine.
The resulting reduction in peripheral sympathetic activity decreases vascular tone and cardiac stimulation, producing a reduction in blood pressure.
Guanethidine was developed primarily for the treatment of hypertension, particularly severe hypertension. Its use has declined substantially because newer antihypertensive medicines have more favorable safety and tolerability profiles.
The antihypertensive action of guanethidine is associated with depletion and inhibition of peripheral norepinephrine release. This reduces sympathetic vasoconstrictor activity and can lower both vascular resistance and blood pressure.
Guanethidine is a synthetic, strongly basic guanidine-containing compound. The free compound has the molecular formula C10H22N4O2 and molecular weight 230.31 g/mol. Pharmaceutical preparations may use the sulfate salt to provide a suitable solid form.
Guanethidine API quality evaluation may include:
Guanethidine should be stored in a tightly closed container under controlled pharmaceutical conditions and protected from excessive heat, moisture and direct light. Exact storage conditions should follow validated stability data and the applicable product-specific specification.
Guanethidine remains relevant as a reference compound for research involving peripheral sympathetic neurotransmission, norepinephrine transport and adrenergic neuron blockade.
Guanethidine is a peripheral adrenergic neuron-blocking agent with CAS Number 55-65-2, molecular formula C10H22N4O2, and molecular weight 230.31 g/mol. It was historically used as an antihypertensive by reducing peripheral norepinephrine release and sympathetic activity.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |