So I've looked around for accessible vasodilators to help relieve the vasoconstriction caused by stimulant use without finding anything too useful. Things like yohimbe, Kratom, Cayenne Pepper, Cannabis, Benzodiazapines, Dark Chocolate, Garlic Cloves, etc keep on popping up in my searches but they arent exactly what Im looking for. I have access to a vendor who lists some potentially useful pharmaceuticals that got my interest. They are Clonidine, Phentolamine, and Tolazoline.
Now i know that its never a particularly good idea to mix drugs that may cause potential interactions, but I feel that its at least worth looking into. I have no real knowledge on these drugs and Id like your help with some hypothesizing. Ill list a brief bit on each one and hope you guys can help with the rest. I really do wish I could look more into them myself but I just dont have the time anymore, unfortunately. From my brief look Id have to say Phentolamine is the best bet, but Im really just guessing.
Clonidine
- a sympatholytic medication used to treat medical conditions, such as high blood pressure
- It is classified as a centrally acting α2 adrenergic agonist
- It can alleviate opioid withdrawal symptoms by reducing the sympathetic nervous system response such as tachycardia and hypertension, as well as reducing sweating, hot and cold flushes, and general restlessness.
- Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases cardiac output and peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, and inhibits the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.
- It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a negative feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, clonidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels.
Phentolamine
- It is a reversible, nonselective alpha-adrenergic antagonist.
- Its primary action is vasodilation due to α1 blockade.
- It also can lead to reflex tachycardia because of hypotension and α2 inhibition, which increases sympathetic tone.
- The primary application for phentolamine is for the control of hypertensive emergencies
- It also has usefulness in the treatment of cocaine induced hypertension, where one would generally avoid beta blockers and where calcium channel blockers are not effective
Tolazoline
- It is a non-selective competitive α-adrenergic receptor antagonist.
- It is a vasodilator that is used to treat spasms of peripheral blood vessels.
- It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A agonist drugs such as LSD, DOB and Bromodragonfly.
Now i know that its never a particularly good idea to mix drugs that may cause potential interactions, but I feel that its at least worth looking into. I have no real knowledge on these drugs and Id like your help with some hypothesizing. Ill list a brief bit on each one and hope you guys can help with the rest. I really do wish I could look more into them myself but I just dont have the time anymore, unfortunately. From my brief look Id have to say Phentolamine is the best bet, but Im really just guessing.
Clonidine
- a sympatholytic medication used to treat medical conditions, such as high blood pressure
- It is classified as a centrally acting α2 adrenergic agonist
- It can alleviate opioid withdrawal symptoms by reducing the sympathetic nervous system response such as tachycardia and hypertension, as well as reducing sweating, hot and cold flushes, and general restlessness.
- Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases cardiac output and peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, and inhibits the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.
- It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a negative feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, clonidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels.
Phentolamine
- It is a reversible, nonselective alpha-adrenergic antagonist.
- Its primary action is vasodilation due to α1 blockade.
- It also can lead to reflex tachycardia because of hypotension and α2 inhibition, which increases sympathetic tone.
- The primary application for phentolamine is for the control of hypertensive emergencies
- It also has usefulness in the treatment of cocaine induced hypertension, where one would generally avoid beta blockers and where calcium channel blockers are not effective
Tolazoline
- It is a non-selective competitive α-adrenergic receptor antagonist.
- It is a vasodilator that is used to treat spasms of peripheral blood vessels.
- It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A agonist drugs such as LSD, DOB and Bromodragonfly.