Action and Spectrum

Actions and Spectrum:

yohimbine is a compound found in the bark of the African yohimbe tree. It acts as an alpha-2 adrenergic receptor antagonist, which can increase sympathetic nervous system activity and lead to effects such as increased heart rate, blood pressure, and anxiety. Yohimbine is used as a dietary supplement and in some prescription medications for the treatment of erectile dysfunction. It has also been studied for its potential use in treating anxiety and depression, although more research is needed in this area. Yohimbine has a narrow therapeutic index, meaning that the difference between a therapeutic and toxic dose is small, and it can cause side effects such as nausea, dizziness, and tremors at high doses.

Drug Interaction

Adverse Reaction

Frequency Not Defined

Headache

Irritability

Sweating

Anxiety

Nausea

Tachycardia

Black Box Warning

Black Box Warning

The U.S. Food and Drug Administration (FDA) has issued a black box warning for yohimbine, a drug that is commonly used to treat erectile dysfunction and improve athletic performance. The warning is due to the risk of serious adverse effects, including heart attack, seizure, and kidney failure

Contraindication / Caution

Contraindication/Caution:

• Cardiovascular disease: Yohimbine can cause an increase in heart rate and blood pressure, which can be dangerous for individuals with a history of heart disease or hypertension.
• Mental health conditions: Yohimbine can worsen symptoms of anxiety and panic disorders, and may also interact with antidepressant medications.
• Kidney or liver disease: Yohimbine can affect the function of these organs, so caution should be exercised in individuals with existing kidney or liver disease.
• Pregnancy and breastfeeding: The safety of yohimbine has not been established in pregnant or breastfeeding women, so it should be avoided.

Medications: Yohimbine can interact with a variety of medications, including antidepressants, blood pressure medications, and drugs that affect the central nervous system. It is important to check with a healthcare provider before taking yohimbine in combination with other medications.

Pregnancy / Lactation

Pregnancy warnings:   

Pregnancy category: N/A

Lactation: Excreted into human milk is unknown

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

yohimbine is an alkaloid compound derived from the bark of the Pausinystalia yohimbe tree. It is a selective antagonist of the alpha-2 adrenergic receptor, which leads to an increase in sympathetic activity and subsequent vasoconstriction. The primary pharmacological effects of yohimbine are related to its ability to increase the release of norepinephrine and inhibit its reuptake.

Pharmacodynamics:

yohimbine works as an alpha-2 adrenergic receptor antagonist, which means it blocks the activity of certain receptors in the body that regulate the sympathetic nervous system. This, in turn, leads to an increase in the release of norepinephrine, a neurotransmitter that can have various effects on the body. Pharmacokinetics:

Absorption

yohimbine is rapidly and completely absorbed from the gastrointestinal tract after oral administration, with a peak plasma concentration achieved within 45 to 90 minutes. Food may delay the absorption but does not affect the extent of absorption.

Distribution

yohimbine is highly protein-bound (about 98%) and has a large apparent volume of distribution. It readily crosses the blood-brain barrier and can also be detected in breast milk.

Metabolism

yohimbine is primarily metabolized in the liver by the cytochrome P450 enzyme system. Its major metabolites are 11-hydroxy-yohimbine and 11-hydroxy-yohimbine glucuronide, which are less potent than the parent compound.

Elimination and Excretion

yohimbine and its metabolites are excreted in the urine, with about 90% of the dose being eliminated within 24 hours. The elimination half-life is about 2.5 to 3 hours. Yohimbine is not recommended for individuals with kidney or liver disease.

Adminstartion

Administration:

Orally administration

yohimbine can be administered orally as a tablet or capsule, or injected intravenously under medical supervision. The dosage and frequency of administration vary depending on the condition being treated and the individual’s response to the medication. It is important to follow the instructions provided by a healthcare professional and to report any side effects or adverse reactions.

Patient Information Leaflet

Patient information leaflet

Generic Name: yohimbine

Why do we use yohimbine?

yohimbine is used for a variety of purposes, but most commonly it is used for its effects on sexual dysfunction and weight loss. yohimbine is thought to work by blocking certain receptors in the body that can interfere with sexual arousal, which may improve symptoms of erectile dysfunction. It may also increase the release of certain hormones that can stimulate fat breakdown and help with weight loss.