Zuellig Pharma
Full Prescribing Info
Each 0.2- and 0.4-mg film-coated tablet contains also the following excipients: Lactose monohydrate, povidone K25, crospovidone, magnesium stearate, hypromellose, ethylcellulose, macrogol 6000, talc, red ferric oxide (E172) and titanium dioxide (E171).
Pharmacotherapeutic Group: Imidazoline receptor agonists.
Pharmacology: Pharmacodynamics: In different animal models, moxonidine has been shown to be a potent antihypertensive agent. Available experimental data suggest that the site of the antihypertensive action of moxonidine is the central nervous system (CNS). Within the brainstem, moxonidine has been shown to selectively stimulate imidazoline receptors. These imidazoline-sensitive receptors are concentrated in the rostral ventrolateral medulla, an area critical to the central control of the peripheral sympathetic nervous system. Stimulation of the imidazoline receptors appears to reduce sympathetic activity and lower blood pressure.
Moxonidine distinguishes itself from other sympatholytic antihypertensives by exhibiting only low affinity for known α2-adrenoceptors, as compared to imidazoline receptors. This low affinity to α2-adrenoceptors may account for a low incidence of sedation and dry mouth with moxonidine.
In humans, moxonidine leads to a reduction of systemic vascular resistance and consequently arterial blood pressure. The antihypertensive effect of moxonidine has been demonstrated in double-blind, placebo-controlled, randomized studies.
In therapeutic trial of 2 months' duration, moxonidine improved the insulin sensitivity index by 21% (decreased symptoms related to insulin resistant diabetes) in comparison to placebo obese and insulin resistant patients with moderate hypertension.
Pharmacokinetics: Absorption: After oral administration, moxonidine component is rapidly (tmax around 1 hr) and almost completely absorbed from the upper gastrointestinal tract. The absolute bioavailability (amount of drug that reaches the blood stream unchanged) is about 88%, indicating no significant first-pass (liver) metabolism. Food intake has no influence on the pharmacokinetics of moxonidine.
Distribution: Plasma protein-binding, as determined in vitro, was about 7.2%.
Biotransformation: In pooled human plasma samples, only dehydrogenated moxonidine was identified. The pharmacodynamic activity of dehydrogenated moxonidine is about 1/10 compared to moxonidine.
Elimination: Over a 24-hr period, 78% of the total dose was excreted in urine as parent moxonidine and 13% of the dose was excreted as dehydrogenated moxonidine. Other minor metabolites in urine accounted for approximately 8% of the dose. Less than 1% is eliminated via the faeces. The elimination half-lives of moxonidine and its metabolite are approximately 2.5 and 5 hrs, respectively.
Hypertensive Patients: In hypertensive patients, no relevant pharmacokinetic changes were observed compared to healthy volunteers.
Elderly: Age-related changes in pharmacokinetics have been observed and are most likely due to a reduced metabolic activity and/or slightly higher bioavailability (better absorption into the blood stream) in the elderly. However, these pharmacokinetic differences are not considered to be clinically relevant.
Children: As Physiotens is not recommended for use in children, no pharmacokinetic studies have been performed in this subpopulation.
Renal Impairment: Elimination of moxonidine is significantly correlated with creatinine clearance (CrCl). In patients with moderate renal impairment glomerular filtration rate (GFR 30-60 mL/min) steady-state plasma concentrations and terminal half-life are approximately 2-fold and 1.5-fold higher, respectively, compared to hypertensive patients with normal renal function (GFR >90 mL/min). In patients with severe renal impairment (GFR <30 mL/min), steady state plasma concentrations and terminal half-life are approximately 3-fold higher. No expected drug accumulation after multiple dosing was observed in these patients. In end-state renal patients (GFR <10 mL/min), undergoing hemodialysis plasma concentrations and terminal half-life are 6- and 4-fold higher, respectively. In all groups, maximum moxonidine plasma concentrations are only 1.5-2 fold higher.
In patients with renal impairment, the dosage and frequency of dosage should be adjusted according to the individual requirements.
Moxonidine is eliminated to a small extent by hemodialysis.
Treatment of hypertension.
Dosage/Direction for Use
Usual Initial Dose: 0.2 mg daily, with a maximum daily dose of 0.6 mg given as 2 divided doses. The maximum single dose to be administered is 0.4 mg. Adjustments in daily dose should be individualized to the patient's response.
Moderate to Severe Renal Impairment and Hemodialysis (Mechanical Cleaning of the Blood): Starting Dose: 0.2 mg daily. If necessary and well tolerated, the physician may then decide to increase the dose to 0.4 mg daily.
Administration: Moxonidine can be administered with or without food. Do not take double dose to compensate for missed tablet(s).
Symptoms: Very few cases of overdose have been reported. However, in one such report, a dose of 19.6 mg was ingested acutely without fatality. Signs and symptoms reported included: Headache, sedation, somnolence (sleepiness), hypotension (low blood pressure), dizziness, asthenia (general weakness), bradycardia (slow resting heart rate), dry mouth, vomiting, fatigue and upper abdominal pain (stomach pain).
In addition, based on a few high-dose studies in animals, transient hypertension (high blood pressure), tachycardia (elevated heart rate) and hyperglycemia (elevated blood sugar) may also occur.
Treatment: No specific antidote is known. In case of hypotension, circulatory support eg, fluids and dopamine administration may be considered. Bradycardia may be treated with atropine. Alpha receptor antagonists may diminish or abolish the paradoxical hypertensive effects of a moxonidine overdose.
Patients with known hypersensitivity to moxonidine or any of the components of Physiotens; sick sinus syndrome (heart arrhythmia due to sinus node disease) or bradycardia (resting HR <50 bpm).
Special Precautions
If moxonidine is used in combination with a β-blocker and both treatments have to be discontinued, the β-blocker should be discontinued first, and moxonidine only thereafter.
Treatment with moxonidine should not be discontinued abruptly. A gradual decrease in dose is recommended before complete discontinuation.
Patients with an intolerance to galactose (eg, Lapp lactase deficiency or glucose-galactose malabsorption) should not take Physiotens as it contains lactose.
Effects on the Ability to Drive or Operate Machinery: No studies on the effects of Physiotens on the ability to drive and/or use machinery have been performed. However, since somnolence (sleepiness) and dizziness have been reported, this should be borne in mind when performing these tasks.
Use in pregnancy & lactation: There are no studies with moxonidine in pregnant women. Because of limited experience in humans, Physiotens should be used in pregnancy only when potential benefit justifies potential risk to the fetus. No congenital effects on reproduction have been observed in preclinical studies.
Moxonidine is excreted in breast milk. Lactating women should be advised not to breastfeed while on moxonidine or stop treatment with the drug.
Use in children: Due to lack of data on safety and efficacy, Physiotens is not recommended for use in children and adolescents <18 years.
Use In Pregnancy & Lactation
There are no studies with moxonidine in pregnant women. Because of limited experience in humans, Physiotens should be used in pregnancy only when potential benefit justifies potential risk to the fetus. No congenital effects on reproduction have been observed in preclinical studies.
Moxonidine is excreted in breast milk. Lactating women should be advised not to breastfeed while on moxonidine or stop treatment with the drug.
Adverse Reactions
Like all medicines, Physiotens may have side-effects.
The frequencies of study related adverse reactions ranked according to the following: Common: Between 1 and 10 cases in 100 treated patients; uncommon: <1 case in 100 treated patients; rare: <1 case in 1000 treated patients; very rare: <1 case in 10,000 treated patients.
The most frequent adverse reactions reported by those taking Physiotens include dry mouth, headache, dizziness, asthenia (general weakness) and somnolence (sleepiness). These symptoms often decrease after the 1st few weeks of treatment.
Adverse Effects by System Organ Class: Nervous System Disorders: Common: Headache, dizziness, somnolence (sleepiness). Uncommon: Insomnia.
Vascular Disorders: Rare: Hypotension (low blood pressure), orthostatic hypotension.
Gastrointestinal Disorders: Common: Dry mouth. Uncommon: Nausea.
Skin and Subcutaneous Tissue Disorders: Uncommon: Rash, pruritus (itchiness). Very Rare: Angioedema (sudden swelling of the face, neck extremities).
General Disorders and Administration Site Reactions: Common: Asthenia (general weakness).
Drug Interactions
Physiotens has been safely administered with other hypertensive drugs (drugs that lower blood pressure) eg, thiazide diuretics and calcium-channel blockers. Joint administration of Physiotens with these and/or other antihypertensive agents results in an additive effect (the total effect of the medication is not higher than the sum effect of each individual medication).
In healthy volunteers, no pharmacokinetic interactions (alterations in absorption, action, metabolism or elimination) have been observed between Physiotens and hydrochlorothiazide, glibenclamide (glyburide), or digoxin.
Since tricyclic antidepressant may reduce the effectiveness of centrally acting antihypertensive agents (eg, Physiotens), it is not recommended that tricyclic antidepressants be jointly administered with Physiotens.
No pharmacodynamic interactions has been demonstrated with moclobemide (a medicine commonly used to treat depression and social anxiety).
Physiotens may enhance the sedative effect of benzodiazepines (sedatives) when administered concomitantly. Furthermore, Physiotens moderately enhances the impaired performance in cognitive functions in patients taking lorazepam (a benzodiazepine class sedative). If you are taking Physiotens at the same time as a benzodiazepines class sedative, you should be aware of the possibility of increased drowsiness (see Effects on the Ability to Drive or Operate Machinery under Precautions).
Incompatibilities: Not applicable.
0.2 mg: Do not store above 25°C.
Shelf-Life: 2 years
0.4 mg: Do not store above 30°C.
Shelf-Life: 3 years.
MIMS Class
Other Antihypertensives
ATC Classification
C02AC05 - moxonidine ; Belongs to the class of imidazoline receptor agonists, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
FC tab 0.2 mg (light pink, round, convex with a stamp "0.2" on one face) x 28's. 0.4 mg (dull red, round, convex with a stamp "0.4" on one face) x 28's.
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