Is it Safe to Use Clonidine in Children?

Clonidine patch, the indication is Clonidine Hydrochloride, which is suitable for the treatment of hypertension. It can be used alone or in combination with other antihypertensive drugs.

Drug Name: Clonidine patch

Drug type: Prescription drugs, external drugs
Use classification: Sympathetic inhibitor

Clonidine patch drug name

[Common name] Clonidine patch

[English name] Clonidine Adhesive Patch

[Chinese Pinyin] Ke Le Ding Tie Pian

Clonidine patch category

Chemical Drugs and Biological Products >> Circulatory Drugs >> Antihypertensive Drugs >> Sympathetic Inhibitor

Clonidine patch ingredients

The main ingredient of this product is clonidine.

Chemical name: 2-[(2,6-dichlorophenyl) imino] imidazolidine

Molecular formula: C ₉ H ₉ N ₃ Cl ₂

Molecular weight: 230.10

Clonidine patch properties

This product is a round or square patch with an adhesive film on the application surface.

Clonidine patch indications

Clonidine hydrochloride is suitable for the treatment of hypertension. It can be used alone or in combination with other antihypertensive drugs.

Clonidine patch specifications

2.5mg

Clonidine patch usage dosage

Take this product, remove the protective layer, and stick it to the ear without dry skin. Adult patients use 1 tablet (2.5cm ² ) for the first time, and then adjust the area (reduction or increase) each time according to the blood pressure drop. If it has been increased to 3 tablets (7.5 cm ² ), it still has no effect and the adverse reactions are obvious. Discontinuation should be considered. Replace with a new patch 3 days after application.

Clonidine patch adverse reactions

Most adverse reactions are mild and there is a tendency to decrease with continuous treatment. The most common (whose appearance is dose-related) are dry mouth (about 40%), doze (about 33%), dizziness (about 16%), constipation (about 10%), and sedation (about 10%).
According to reports, among patients taking clonidine hydrochloride at the same time, very few patients have the following adverse reactions, and the causal relationship between the drug and these adverse reactions has not been determined.
1. Systemic reactions are weak (about 10%), fatigue (about 4%), headache (about 1%), and withdrawal syndrome (about 1%). In addition, pale; weak positive of the Cums test; increased sensitivity to alcohol and fever.
2. The cardiovascular system occasionally has orthostatic symptoms (about 3%), palpitations and tachycardia (about 0.5%), and bradycardia (about 0.5%). Raynaud's phenomenon, congestive heart failure, and abnormal electrocardiograms (ie, sinus node suppression, functional bradycardia, excessive AV block, and arrhythmia). Sinus node bradycardia and atrioventricular block were occasionally seen in rare cases with and without digoxin.
3 Central nervous system nervousness and agitation (about 3%), depression (about 1%), and insomnia (about 0.5%). Occasional behavior changes, fantasy or nightmares, restlessness, anxiety, audiovisual hallucinations, and delirium.
4 Dermatological rash (about 1%), pruritus (about 0.7%), urticaria and angioedema (about 0.5%), and hair loss (about 0.2%).
5. Gastrointestinal nausea and vomiting (about 5%), anorexia (about 1%) and gastrointestinal discomfort (about 1%), mild short-term liver function abnormalities (about 1%), occasional hepatitis, mumps, constipation , False obstruction and abdominal pain.
6. Reproductive activity in the genitourinary system decreases, impotence and loss of libido (approximately 3%); nocturia (approximately 1%); difficulty urinating (approximately 0.2%); urinary retention (approximately 1%).
7. Hematology occasionally has thrombocytopenia.
8. Metabolic weight gain (approximately 1%), male and female breasts (approximately 0.1%), occasional short-term increases in blood glucose or serum creatine phosphokinase.
9. Muscle and skeletal muscle or joint pain (about 0.6%) and leg cramps (about 0.3%).
10 Mouth-otolaryngology occasionally see dry nasal mucosa.
11. Ophthalmology Dry eyes, burning eyes, and blurred vision.

Clonidine patch taboo

Those who are known to be allergic to clonidine are contraindicated.

Clonidine patch notes

1. In general, patients who are sensitized by local contact with clonidine patch, continuous treatment with clonidine patch or oral clonidine hydrochloride may produce a general rash.
For patients with allergic reactions to clonidine patches, oral clonidine hydrochloride may also cause allergic reactions (including general rash, urticaria, or angioedema).
Patients with severe coronary atresia, conduction disorders, recent myocardial infarction, cerebrovascular disease, or chronic renal failure should be treated with caution.
2. Intraoperative administration of nicardipine hydrochloride should be continued until the start of surgery and resumed as soon as possible after surgery. Blood pressure should be carefully monitored during surgery and other measures should be taken to control blood pressure if needed.
3 Patient information Patients should be careful with medication and do not interrupt treatment without the doctor's permission.
Patients engaged in hazardous activities such as operating a machine or driving a car should be aware of the possible sedative effects of clonidine. It should also be known that this sedative effect can be enhanced by concomitant use of alcohol, barbiturates or other sedatives.
4 Patients should be discontinued without discontinuing treatment without the doctor's permission. In some cases, abrupt discontinuation of clonidine treatment can cause complications such as nervousness, agitation, headaches, and tremors, or lead to a rapid rise in blood pressure and increased plasma catecholamine concentrations. Interruption of clonidine treatment after higher doses or in combination with beta-blockers appears to be more likely to occur, so special care should be taken in these cases. After clonidine discontinuation, hypertensive encephalopathy, cerebrovascular accident, and death occurred in a few cases. When discontinuing clonidine hydrochloride treatment, the dose should be gradually reduced over a period of 2 to 4 days to avoid withdrawal syndrome.
Hypertension caused by interrupting clonidine hydrochloride therapy can be reversed by oral clonidine hydrochloride or intravenous phentolamine. If the combination of beta-blocker and clonidine is to be discontinued, the beta-blocker should be discontinued a few days before clonidine hydrochloride is gradually discontinued.
Because children often have gastrointestinal disorders that cause vomiting, they may be more sensitive to high blood pressure attacks caused by missed medication.

Clonidine patch for pregnant and lactating women

There is insufficient data on the use of drugs in pregnant women. Therefore, during pregnancy, use it only when it is particularly needed. Because the drug clonidine hydrochloride is secreted in breast milk, care should be taken by lactating women.

Clonidine patch for children

The safety and efficacy of medications for children under 12 years of age have not been determined. (See "Discontinuation" in "Warnings")

Clonidine patch drug interactions

Clonidine may enhance CNS inhibition by alcohol, barbiturates or other sedatives. If patients taking clonidine hydrochloride also take tricyclic antidepressants, the antihypertensive effect of clonidine may be reduced, so the dose needs to be increased.
Clonidine should be used in patients taking clonidine with drugs that affect sinus node function or AV conduction such as digoxin, calcium channel blockers, and beta-blockers, as additive effects such as bradycardia and AV block Stagnation.
Amitriptyline in combination with clonidine promotes corneal damage in mice (see "Toxicology").

Clonidine patch overdose

Hypertension can be caused early and subsequent hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, reduced or no reflex effects, weakness, excitability, and dilated pupils. Children have higher CNS inhibition than adults. Large overdose can cause reversible cardiac conduction defects or rhythm disorders, asphyxia, coma, and seizures. Signs or symptoms of overdose usually appear within 30 minutes to 2 hours after taking the medicine. Children have shown signs of toxicity when taking a 0.1 mg dose of cola.
When clonidine is in excess, there is no specific antidote. An overdose of clonidine can cause rapid CNS suppression; therefore, it is not recommended to induce vomiting with soil roots. Following a recent and / or large dose, gavage may be appropriate. Administration of activated carbon and / or laxatives may also be beneficial. Supportive treatments include bradycardia with atropine sulfate, hypotension with intravenous solutions and / or boosters, and hypertension with vasodilators. Naloxone can be used as an adjunct to clonidine-induced respiratory depression, hypotension, and / or coma; blood pressure should be monitored because naloxone can sometimes cause abnormal hypertension. The results from torazoline administration are inconsistent and not recommended as a first-line treatment. Dialysis does not seem to significantly promote the elimination of clonidine.
The largest overdose reported to date is a 28-year-old man who took 100 mg of clonidine hydrochloride powder. The patient developed hypertension first, followed by hypotension, bradycardia, asphyxia, hallucinations, semi-coma, and extraventricular contractions. Clonidine concentration in plasma: 190 ng / ml after 1 hour, 60 ng / ml after 1.5 hours, 370 ng / ml after 2 hours, and 120 ng / ml after 5.5 and 6.5 hours. In mice and rats, the LD _{50 of} clonidine was 206 mg / kg and 465 mg / kg, respectively.

Clonidine patch pharmacology and toxicology

1. Pharmacological clonidine stimulates brainstem alpha-receptors. This effect causes a reduction in the impulsive transmission of the sympathetic nerves from the central nervous system, thereby reducing peripheral resistance, renal vascular resistance, heart rate, and blood pressure. Clonidine hydrochloride works relatively quickly. Within 30 to 60 minutes after oral administration, the patient's blood pressure began to decrease, and reached a maximum within 2 to 4 hours. Renal blood flow and glomerular filtration rate remained essentially unchanged. Normal orthostatic reflexes are complete; therefore, orthostatic symptoms are mild and rare.
Acute human studies of clonidine hydrochloride have shown that the cardiac output in the supine position is appropriately reduced (15% to 20%), and the peripheral resistance remains unchanged. When the tilt is 45 °, the cardiac output is slightly reduced and the peripheral resistance is reduced. During long-term treatment, cardiac output tends to return to the control value, while peripheral resistance remains reduced. It has been observed that most patients taking clonidine have slowed pulse rates, but the drug does not alter the normal hemodynamic response caused by exercise.
Some patients may develop tolerance to hypotensive effects, so it is necessary to re-evaluate the treatment. Other studies in the human body provide evidence for reduced plasma renin activity and decreased excretion of aldosterone and catecholamines. The exact relationship between these pharmacological effects and the antihypertensive effect of clonidine has not been fully elucidated.
Clonidine strongly stimulates the release of growth hormone in children and adults, but long-term use does not cause a chronic increase in growth hormone.
2. Toxicity In a study of oral clonidine hydrochloride for 6 months or more in rats, a dose-dependent increase in the incidence and severity of spontaneous retinal degeneration was seen. Studies of tissue distribution in dogs and monkeys have shown clonidine in the choroid.
Considering that retinal degeneration was seen in rats, during the clinical trial, 908 patients had their eyes inspected before and after treatment with clonidine. Of these, 353 patients were examined for more than 24 months or longer. Except for some people with dry eyes, no drug-related ophthalmic abnormalities were found, and according to professionally designed tests such as retinal plethysmography, there was no change in retinal function.
When combined with amitriptyline, clonidine hydrochloride caused corneal damage in rats within 5 days.
3 Carcinogenicity, mutagenicity and reproductive toxicity Long-term through the diet at 46 or 70 times the recommended maximum daily dose (9 or 6 times the MRDHD in mg / m ² ), respectively Rats (132 weeks) or mice (78 weeks) given clonidine showed no carcinogenic effect. No reproductive toxicity was seen in the Ames mutagenicity test. Clonidine at doses up to 150 mcg / kg (approximately 3 times MRDHD) did not affect fertility in male or female rats. In separate trials performed by males and females, at a dose of 500-2000 mcg / kg (10-40 times MRDHD in mg / kg; 2-8 in MRDHD in mg / m ² ) Fertility seems to be affected.

Clonidine patch pharmacokinetics

In about 3 to 5 hours, the plasma concentration of clonidine reaches a peak, and the plasma half-life (t _1/2 ) is 12 to 16 hours. Patients with severe renal impairment have increased plasma half-life to 41 hours. After oral administration, within 24 hours, about 40% to 60% of the absorbed dose is excreted in the urine as the original drug. Approximately 50% of the absorbed dose is metabolized in the liver.