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Last Updated on June 3, 2023

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The active ingredient Clonidine is used therapeutically diverse, such as the treatment of hypertension, withdrawal symptoms in drug or alcohol addiction, migraine and glaucoma (glaucoma). Due to the many points of attack in the body but it can also lead to adverse effects of therapy. Here you can read everything worth knowing about Clonidine: mode of action, use and possible side effects

How Clonidine works

Clonidine acts in the human nervous system as so-called sympatholytic, so it inhibits the action of the sympathetic nervous system. This is the part of the autonomic nervous system, which puts the body using the “stress hormone” adrenaline and noradrenaline in increased willingness to perform – ie body reactions such as rapid heartbeat, a bronchodilator (better oxygen uptake) and a rise in blood pressure triggers. This condition is also called “fight or flight” mode (English “fight or flee” for). The opponent for the sympathetic nervous system is the parasympathetic nervous system: It ensures the regeneration of the body and aids digestion, which is why he also “rest and digest” mode (English for “rest and digest”) is called

The drug Clonidine inhibits the release of “messengers of the sympathetic nervous system, adrenalin and noradrenalin. This ultimately leads to a decrease in blood pressure and heart rate, a slight sedative and pain relief.

Pharmacokinetics and metabolism of Clonidine

After taking a tablet of Clonidine is well absorbed through the intestinal wall into the bloodstream and reaches its maximum blood levels after one to three hours. In the liver, a small part of the administered amount of drug is degraded by enzymes. After about five to 25 hours half of the administered amount of Clonidine three-quarters in the urine and to a quarter of the chair has resigned.

When is Clonidine used?

The drug Clonidine can be officially used:

  • to treat
  • in emergency medicine at hyperactive sympathetic nervous system, which is accompanied by tremors, and restlessness
  • to alleviate withdrawal symptoms in the treatment of drug or alcohol addiction
  • to treat glaucoma (glaucoma)

In addition, Clonidine is currently “off-label”, ie, used for other than the permitted uses.

Usually, the application is carried out in the longer term.

How Clonidine is taken?

In general, Clonidine is taken in the form of tablets or capsules, especially for the treatment of hypertension. At the beginning of treatment, the dosage is gradually increased until the individual dose requirements is found – this procedure is called also “creeping dose”. Another advantage of this slow dose escalation is that it does not come as too much blood pressure drops, which become noticeable as dizziness or weakness.

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To be taken twice daily (morning and evening), unless Retardkapseln be taken, which release the active ingredient Clonidine slowly throughout the day. Then, a once daily intake is sufficient. Usual daily doses will be between 150 and 600 micrograms Clonidine, the maximum dose is 900 micrograms. However, up to 1800 micrograms Clonidine come for very severe cases of hypertension in exceptional cases to use.

Especially for use in glaucoma (glaucoma), there are also eye drops containing the active ingredient Clonidine. Here, depending on a drop in the affected eye is given two to three times daily. Contact lenses and other eye drops or ointments should be used only if at least 15 minutes after that.

What are the side effects of Clonidine?

In the treatment with Clonidine it comes with more than one out of ten patients dizziness (including when getting up), an attenuation of the nervous system, and dry mouth.

In addition, show up at one of tens to hundreds of patients treated Clonidine side effects such as depression, insomnia, nausea, vomiting, sore salivary glands, erectile dysfunction (impotence) and fatigue.

What should I watch for while taking Clonidine?

In combination with other antihypertensive agents can lead to increased blood pressure. Examples of such agents are:

  • the beta blockers Metoprolol and Bisoprolol (cardiovascular agent)
  • the dehydrating agents (diuretics) Furosemide, Hydrochlorothiazide and Spironolactone
  • the ACE inhibitor Captopril, Enalapril and Ramipril)
  • the vasodilator active ingredient Alfuzosin, Doxazosin and Tamsulosin

In contrast pressor substances reduce the effect of Clonidine. Such substances are, for example:

  • large amounts of sodium (such as those found in saline or table salt)
  • certain rheumatic and painkillers (aspirin / acetylsalicylic acid, Ibuprofen, Diclofenac, piroxicam, Etoricoxib)
  • Amitriptyline (antidepressant)
  • certain remedy for mental disorders (antipsychotics / neuroleptics such as chlorpromazine, haloperidol, clozapine)

The concomitant use of drugs that have a calming effect, leading to increased sedative effect. The same is true with simultaneous alcohol consumption.

In general: The combination of Clonidine with other drugs should always be previously discussed with the doctor or pharmacist

In some cases, Clonidine “off-label” in combination with methylphenidate in children and adolescents with attention-deficit (hyperactivity) disorder (ADHD) was used, which had serious and sometimes fatal side effects. From this combination of active substances is therefore not recommended strictly.

For use in children and adolescents have not been studied, and therefore the use is not recommended. Also pregnant and nursing mothers should not take Clonidine, because it crosses the placenta and is excreted into breast milk.

In the elderly (over 65 years) and patients with severe renal impairment is possibly a lower Clonidine dose needed.

If the therapy is to be terminated, Clonidine should not be discontinued suddenly. Instead, the dosage should be reduced gradually and step by step (tapering of dose). Otherwise, it can cause a sudden and very strong rise in blood pressure occur (so-called “rebound” phenomenon).

How to obtain medication with Clonidine

After a doctor’s prescription to obtain preparations containing the active ingredient in Clonidine dosage requirements in the pharmacy.

Since when Clonidine is known?

In the early 1960s it was discovered during testing of various substances to the decongestion of the nasal mucosa that a substance – Clonidine – has a strong antihypertensive effect. After further investigation, the active ingredient was first approved in 1970 as a means for lowering blood pressure. Since the patent has since expired, there are now several generic (generic preparations of the original) with the active ingredient Clonidine .