Clonidine Hydrochloride
Clonidine hydrochloride powder is an antihypertensive drug. It is primarily used to treat migraine, severe dysmenorrhea, menopausal hot flashes, glaucoma, and moderate to severe hypertension, as well as hypertension combined with glaucoma. It can be taken alone or with other medications that reduce blood pressure. The plasma concentration of clonidine peaks at approximately 3-5 hours, and the plasma half-life is 12-16 hours. The plasma half-life increases to 41 hours in patients with severe renal impairment. Within 24 hours of administration, 40–60% of the absorbed dose is eliminated as an unaltered medication in the urine. The liver metabolizes around half of the absorbed dosage. It acts directly on the central postsynaptic membrane α-2 receptors in the hypothalamus and medulla oblongata, activating inhibitory neurons and reducing the outgoing of central sympathetic nerve impulses, inhibiting peripheral sympathetic nerve activity. In addition, it can also act on α-2 receptors on the presynaptic membrane of peripheral sympathetic nerves, enhance their negative feedback effect, reduce the release of norepinephrine from peripheral nerves, reduce peripheral vascular and renal vascular resistance, slow down the heart rate and lower blood pressure. So, If you are interested in antihypertensive drugs, please feel free to contact Xi'an Sonwu. Xi'an Sonwu can provide you with pure clonidine Hcl.
What Is The Mechanism Of Action Of Clonidine Hydrochloride
1. Mechanism
Clonidine Hcl is an α-receptor agonist, which directly stimulates the central postsynaptic membrane α2 receptors in the hypothalamus and oblongata, excitating inhibitory neurons, reducing the outgoing of central sympathetic nerve impulses, thereby inhibiting peripheral sympathetic nerve activity. Additionally, it increases the negative feedback effect of peripheral sympathetic nerve stimulation, enhances α2 receptors on the presynaptic membrane of peripheral vessels, decreases peripheral and renal vascular resistance, slows down heart rate, and lowers blood pressure. There was hardly any change in the renal blood flow or the glomerular filtration rate. Orthostatic symptoms are mild or rare, and orthostatic hypotension rarely occurs. Clonidine Hcl causes a moderate (15% to 20%) reduction in supine cardiac output without changing peripheral vascular resistance.
2. Mechanism of action at the molecular level
Clonidine Hcl acts as a selective agonist of alpha-2 receptors, binding to these receptors in the brain and spinal cord and mimicking natural alpha-2 receptor agonism. This agonistic effect results in specific biological effects, including vasodilation and a decrease in heart rate.
3. Role in the overall physiological system
The effects of clonidine hydrochloride in the overall physiological system involve the following processes:
Sympathetic Nervous System Inhibition: By activating alpha-2 receptors, clonidine Hcl suppresses sympathetic nervous system activity. This inhibition results in inhibited release of norepinephrine, thereby reducing sympathetic nervous system stimulation of the cardiovascular system, including the heart and blood vessels.
Reduce vascular resistance: The action of clonidine hydrochloride relaxes vascular smooth muscles, resulting in a reduction in peripheral vascular resistance. That promotes blood vessel dilation and helps lower blood pressure.
Slows down heart rate: Clonidine Hcl reduces the contractility and heart rate of the heart through its action. That lessens the strain the heart puts on the circulatory system, which decreases the heart's workload and lowers blood pressure.
4. Effects on other physiological systems
In addition to treating hypertension, it may also have effects on other physiological systems, such as:
Central Nervous System: Clonidine Hcl may affect the central nervous system, causing drowsiness and sedation.
Other potential effects: The impact of clonidine hydrochloride may also be related to different physiological and pathophysiological processes, such as pain modulation and attention deficit hyperactivity disorder.
What Is Clonidine Hydrochloride Used For
1. Hypertension (High Blood Pressure)
Clonidine Hcl is commonly prescribed to treat high blood pressure. It lowers the activity of the sympathetic nervous system, which causes vasodilation and a drop in blood pressure.
2. Attention Deficit Hyperactivity Disorder (ADHD)
It is sometimes used off-label to manage symptoms of ADHD, particularly in individuals who may not respond well to or tolerate stimulant medications commonly prescribed for ADHD.
3. Anxiety Disorders
Clonidine Hcl may be used in the treatment of specific anxiety disorders due to its soothing effects. It can help alleviate symptoms of anxiety, although it's not typically considered a first-line treatment for anxiety disorders.
4. Opioid Withdrawal
Sometimes, the symptoms of opioid withdrawal, including anxiety, agitation, sweating, and high blood pressure, can be relieved by it. It can help manage withdrawal symptoms and facilitate detoxification in individuals undergoing opioid withdrawal.
5. Tourette Syndrome
In some cases, it may be prescribed to manage tics associated with Tourette syndrome, particularly when other treatments have been ineffective or not well tolerated.
6. Menopausal Symptoms
Clonidine Hcl may be used to alleviate hot flashes and other menopausal symptoms in women.
Is Clonidine Hydrochloride Safe
Most side effects are minimal and usually go away if medication is sustained. The most common (their occurrence is dose-related) are dry mouth, drowsiness, dizziness, constipation, and sedation. It has been reported that a minimal number of patients who took clonidine hydrochloride at the same time had the following adverse reactions. The causal relationship between the drug and these adverse reactions has not been determined.
1. Systemic reactions include weakness; fatigue; headache; and withdrawal syndrome. In addition, paleness, weakly positive Coombs' test, increased sensitivity to alcohol, and fever.
2. Occasionally, orthostatic symptoms of the cardiovascular system include palpitations, tachycardia, and bradycardia, raynaud's phenomenon, congestive heart failure, and electrocardiographic abnormalities (i.e., sinoatrial node suppression, functional bradycardia, excessive AV block, and arrhythmias). Sinoatrial bradycardia and atrioventricular block have occasionally been reported in rare cases with and without concomitant use of digoxin.
3. Nervousness and excitement in the central nervous system; mental depression and insomnia. Occasionally, behavioral changes, hallucinations or nightmares, restlessness, anxiety, audiovisual hallucinations, and delirium may occur.
4. Dermatological rash; pruritus; urticaria and angioedema; alopecia.
5. Gastrointestinal nausea and vomiting; anorexia and gastrointestinal discomfort; mild short-term liver function test abnormalities; occasionally hepatitis, mumps, constipation, pseudo-obstruction, and abdominal pain.
6. Reduced sexual activity, impotence, and loss of sexual desire in the genitourinary system; nocturia; difficulty urinating; urinary retention.
7. Thrombocytopenia is occasionally seen in hematology.
8. Metabolic weight gain; gynecomastia; occasional short-term blood sugar elevation or serum creatine phosphokinase.
9. Muscle and skeletal muscle or joint pain and leg cramps.
10. Dry nasal mucosa is occasionally seen in the Department of Oral, Otolaryngology, and Otolaryngology.
11. Ophthalmology: Dry eyes, eye-burning sensation, and blurred vision.
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