Clonidine

Chemical formula: C₉H₉Cl₂N₃  Molecular mass: 230.094 g/mol  PubChem compound: 2803

Interactions

Clonidine interacts in the following cases:

Alpha 2 receptor blockers

Substances with alpha2-receptor blocking properties, such as mirtazapine, may abolish the alpha2-receptor mediated effects of clonidine in a dose-dependent manner.

Alpha-1 blockers

Clonidine should not be administered concomitantly with alpha1-adrenergic receptor blockers.

Tricyclic antidepressants, neuroleptics

The antihypertensive effect of clonidine may be reduced or abolished and orthostatic hypotension may be provoked or aggravated by concomitant administration of tricyclic antidepressants or neuroleptics with alpha-receptor blocking properties.

Antihypertensive agents

The reduction in blood pressure induced by clonidine can be further potentiated by concurrent administration of other hypotensive agents. This can be of therapeutic use in the case of other antihypertensive agents such as diuretics, vasodilators, beta-receptor blockers, calcium antagonists and ACE-inhibitors, but the effect of alpha-1 blockers is unpredictable.

Beta-receptor blockers, digitalis glycosides

Concomitant administration of substances with a negative chronotropic or dromotropic effect such as beta-receptor blockers or digitalis glycosides can cause or potentiate bradycardic rhythm disturbances.

It cannot be ruled out that concomitant administration of a beta-receptor blocker will cause or potentiate peripheral vascular disorders.

Non-steroidal anti-inflammatory agents

Substances which raise blood pressure or induce a sodium ion (Na+) and water retaining effect such as non-steroidal anti-inflammatory agents can reduce the therapeutic effect of clonidine.

Haloperidol

Based on observations in patients in a state of alcoholic delirium it has been suggested that high intravenous doses of clonidine may increase the arrhythmogenic potential (QT-prolongation, ventricular fibrillation) of high intravenous doses of haloperidol. Causal relationship and relevance for anti-hypertensive treatment have not been established.

Contact lenses

Patients who wear contact lenses should be warned that treatment with clonidine may cause decreased lacrimation.

Depression, peripheral vascular occlusive disease, cerebrovascular or coronary insufficiency

Clonidine should only be used with caution in patients with depression or a history thereof, with Raynaud’s disease, or other peripheral vascular occlusive disease. The product should only be used with caution in patients with cerebrovascular or coronary insufficiency. Clonidine should also be used with caution in patients with mild to moderate bradyarrhythmia such as low sinus rhythm, and with polyneuropathy or constipation.

Heart failure

As with other antihypertensive drugs, treatment with clonidine should be monitored particularly carefully in patients with heart failure.

Pregnancy

There are limited amount of data from the use of clonidine in pregnant women. This product should only be used in pregnancy if considered essential by the physician. Careful monitoring of mother and child is recommended.

Clonidine passes the placental barrier and may lower the heart rate of the foetus. Post partum a transient rise in blood pressure in the newborn cannot be excluded.

There is no adequate experience regarding the long-term effects of prenatal exposure.

During pregnancy the oral forms of clonidine should be preferred. Intravenous injection of clonidine should be avoided.

Non-clinical studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity.

Nursing mothers

Clonidine is excreted in human milk. However, there is insufficient information on the effect on newborns. The use of clonidine is therefore not recommended during breastfeeding.

Carcinogenesis, mutagenesis and fertility

Fertility

No clinical studies on the effect on human fertility have been conducted with clonidine.

Non-clinical studies with clonidine indicate no direct or indirect harmful effects with respect to the fertility index.

Effects on ability to drive and use machines

No studies on the effects on the ability to drive and use machines have been performed.

However, patients should be advised that they may experience undesirable effects such as dizziness, sedation and accommodation disorder during treatment with clonidine. If patients experience the above mentioned side effects they should avoid potentially hazardous tasks such as driving or operating machinery.

Adverse reactions


Most adverse effects are mild and tend to diminish with continued therapy.

Adverse events have been ranked under headings of frequency using the following convention: Very common ≥/10, Common ≥1/100, <1/10, Uncommon ≥1/1000, <1/100, Rare ≥1/10000, <1/1000, Very rare <1/10000, Not known Cannot be estimated from the available data.

Endocrine disorders

Rare: Gynaecomastia

Psychiatric disorders

Common: Depression, Sleep disorder

Uncommon: Delusional perception, Hallucination, Nightmare

Not known: Confusional state, Libido decreased

Nervous system disorders

Very common: Dizziness, Sedation

Common: Headache

Uncommon: Paraesthesia

Eye disorders

Rare: Lacrimation decreased

Not known: Accommodation disorder

Cardiac disorders

Uncommon: Sinus bradycardia

Rare: Atrioventricular block

Not known: Bradyarrhythmia

Vascular disorders

Very common: Orthostatic hypotension

Uncommon: Raynaud’s phenomenon

Respiratory, thoracic and mediastinal disorders

Rare: Nasal dryness

Gastrointestinal disorders

Very common: Dry mouth

Common: Constipation, Nausea, Salivary gland pain, Vomiting

Rare: Colonic pseudo-obstruction

Skin and subcutaneous tissue disorders

Uncommon: Pruritus, Rash, Urticaria

Rare: Alopecia

Reproductive system and breast disorders

Common: Erectile dysfunction

General disorders and administration site conditions

Common: Fatigue

Uncommon: Malaise

Investigations

Rare: Blood glucose increased

There are occasional reports of fluid retention during initial stages of oral treatment. This is usually transitory and can be corrected by the addition of a diuretic.

Occasional reports of abnormal liver function tests and two cases of hepatitis have also been reported.

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