Actifed

Actifed is a decongestant drug with a systemic effect. It is used to treat diseases in the nasal cavity.

Indications Actifeda

It is used to eliminate pathological symptoms in the upper respiratory tract that occur with diseases such as vasomotor or allergic rhinitis, as well as flu or colds.

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Release form

The drug is released in the form of an oral solution in 0.1 l vials.

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Pharmacodynamics

Triprolidine helps to alleviate the symptoms of the disease in cases where this effect partially or fully depends on the processes of histamine release. The substance is a competitive antagonist (with a powerful therapeutic effect) of the H1-endings of histamine from the alkylamine group. At the same time, it has a minimal anticholinergic effect.

Pseudoephedrine is highly effective in eliminating mucosal edema in the upper part of the respiratory tract, because it is a sympathomimetic with indirect and direct types of influence. Compared to ephedrine, pseudoephedrine is much less likely to increase blood pressure and develop tachycardia, and in addition, it does not stimulate the central nervous system as intensely.

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Pharmacokinetics

Triprolidine and pseudoephedrine are well absorbed through the intestines when taken orally. After taking 1 tablet, the plasma Cmax values of triprolidine are approximately 5.5-6.0 ng/ml; the substance reaches these marks after 2 hours. The half-life of triprolidine is about 3.2 hours. Only about 1% of the portion of triprolidine is excreted unchanged.

Pseudoephedrine Cmax values are approximately 180 ng/mL and require 120 minutes to reach. The half-life of pseudoephedrine is 5.5 hours.

Part of pseudoephedrine is involved in hepatic metabolic processes with the formation of an inactive metabolic product. Pseudoephedrine with its metabolic products is excreted through the kidneys, 55-75% of the portion - in an unchanged state. Pseudoephedrine excretion rates increase in the case of urine acidification (accordingly, they decrease with an increase in the pH level of urine).

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Dosing and administration

The patient should be warned that he/she must contact a doctor if the symptoms of the disease do not disappear after 7 days. It is necessary to strictly follow the doctor's instructions regarding the scheme and dosage. It is forbidden to combine with other medications containing an antihistamine substance (including drugs for the treatment of cough and colds).

For teenagers from 12 years old and adults, the portion is 10 ml with 3-4-times oral use per day. A maximum of 40 ml of the substance is allowed per day.

Children aged 6-11 years are required to take 5 ml of the medicine 3-4 times a day. No more than 20 ml of Actifed is allowed per day.

Children aged 2-6 years are prescribed 2.5 ml of the medicine 3-4 times a day. The maximum possible daily dose is 10 ml.

Portion sizes of drugs for kidney disorders.

Pseudoephedrine is excreted via the kidneys. In renal insufficiency, the plasma pseudoephedrine level increases, so it should not be used in people with severe renal insufficiency. Caution is required when prescribing to people with moderate impairment.

Dosage regimen for liver dysfunction.

Triprolidine is excreted primarily via hepatic metabolism, which is why the need for dosage reduction should be considered in people with severe liver disease.

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Use Actifeda during pregnancy

The medication should not be prescribed to breastfeeding mothers or pregnant women.

Contraindications

Main contraindications:

• the presence of intolerance to pseudoephedrine hydrochloride and triprolidine hydrochloride, as well as acrivastine or other auxiliary components of the drug;
• elevated blood pressure (severe severity);
• Severe coronary heart disease;
• pheochromocytoma;
• severe renal failure;
• severe forms of renal or hepatic pathologies;
• bronchitis, bronchial asthma or bronchiectasis, in which excessive secretion is observed;
• use together with other sympathomimetics (drugs that suppress appetite, decongestants, as well as amphetamine-like psychostimulants);
• use in people who are taking or have taken in the last 14 days MAOIs (this includes the antibacterial drug furazolidone).

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Side effects Actifeda

Adverse effects of pseudoephedrine.

Side effects include:

• Mental disorders: insomnia and a feeling of nervousness are often observed. Sometimes a feeling of restlessness, agitation or tremor is observed. Hallucinations occasionally occur (mainly in children);
• problems in the nervous system: dizziness often appears. Sometimes headaches occur;
• lesions affecting the cardiovascular system: arrhythmia or tachycardia occasionally develops, blood pressure increases, and the heartbeat intensifies. An increase in systolic blood pressure values has also been recorded;
• Gastrointestinal disorders: nausea or vomiting often appear, as well as dry mouth. Sometimes a loss of appetite is noted;
• lesions of the subcutaneous layer and epidermis: hyperhidrosis, allergic dermatitis and rashes are occasionally observed. The use of pseudoephedrine can lead to the appearance of various signs of allergy from the epidermis (may be accompanied by systemic manifestations (Quincke's edema and bronchial spasm) or not);
• disorders affecting the urinary system and kidneys: urinary retention and dysuria are sometimes observed. Urination problems occur mainly in people with obstruction of the urethra (for example, prostatic hypertrophy).

Adverse symptoms of triprolidine.

Among the developing effects:

• mental disorders: paradoxical arousal (most sensitive in older people and children) feelings of restlessness or nervousness and increased energy, feelings of confusion (most common in older people), delirium during sleep and hallucinations (usually in children) may occur;
• lesions affecting the nervous system: a feeling of drowsiness or a sedative effect often appears. Dizziness, inattention and coordination disorder are also quite often recorded. Headaches sometimes occur;
• disturbances in the functioning of the cardiovascular system: sometimes tachycardia, orthostatic collapse and a feeling of weakness occur;
• manifestations from the visual organs: possible development of blurred vision;
• lesions of the ENT organs and sternum organs: nasal congestion and thickening of bronchial secretions are possible;
• gastrointestinal disorders: dryness in the throat, as well as in the oral and nasal mucosa, is common. Discomfort in the gastrointestinal tract (including vomiting with nausea) may occur, as well as constipation, anorexia, heartburn or diarrhea, increased appetite and weight gain;
• disorders associated with the epidermis and subcutaneous layer: photosensitivity, urticaria or rashes may occur;
• problems with the function of the urinary organs and kidneys: polyuria or dysuria may occur, as well as urinary retention.

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Overdose

In case of pseudoephedrine poisoning, symptoms may appear due to stimulation of the cardiovascular system and central nervous system (for example, a feeling of anxiety or excitement, arrhythmia, hallucinations, vomiting, increased blood pressure, increased heart rate, nausea, urinary disorders and a feeling of thirst). In case of severe overdoses, convulsions, psychosis with hypertensive crisis and a comatose state may appear.

A decrease in serum potassium levels is possible due to its transport from the extracellular to the intracellular space.

Triprolidine intoxication will likely cause symptoms similar to the adverse effects of this substance. In addition, a feeling of weakness, tremor, ataxia, dry mucous membranes and epidermis may occur, as well as respiratory depression, psychosis, arrhythmia, hyperpyrexia, tachycardia, and convulsions.

The necessary supportive measures are required to help eliminate the corresponding specific signs. Manifestations of CNS stimulation and seizures are treated by parenteral injection of diazepam. The use of β-blockers eliminates hypokalemia and complications affecting the cardiovascular system.

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Interactions with other drugs

The combination of pseudoephedrine hydrochloride with MAOIs (or taking the drug for 14 days after the end of the course using MAOIs) can lead to the development of a hypertensive crisis. MAOIs also potentiate the cholinolytic activity of triprolidine.

When used in combination with sympathomimetics (such as appetite suppressants, decongestants and amphetamine psychostimulants), which affect the processes of catabolism of sympathomimetic amines, an increase in blood pressure is possible.

Taking it together with sedative or hypnotic drugs, as well as tranquilizers, potentiates the feeling of drowsiness. The same effect is noted when drinking alcoholic beverages while taking the drug.

Pseudoephedrine can have an antagonistic effect when combined with certain antihypertensive medications (for example, methyldopa, guanethidine with reserpine, as well as β-blockers and debricosvin).

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Storage conditions

Actifed must be stored in a dark and dry place, out of the reach of small children. Temperature values should not exceed 25°C.

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Shelf life

Actifed can be used within 4 years from the date of production of the therapeutic drug.

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Application for children

Actifed is prohibited for use in children under 2 years of age.

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Analogues

An analogue of the drug is Trifed.

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