Acknowledge

Aktifed is a decongestant medication with a systemic type of influence. Used to treat diseases in the nasal cavity.

Indications The effect

It is used to eliminate the pathological signs in the upper region of the respiratory tract that occur in diseases such as the vasomotor or allergic rhinitis, and also for flu or a cold.

[1], [2], [3], [4], [5], [6], [7], [8]

Release form

The release of the drug is made in the form of an oral solution in bottles with a volume of 0.1 l.

[9], [10], [11], [12], [13], [14], [15], [16], [17]

Pharmacodynamics

Triprolidine helps alleviate the symptoms of the disease in cases where this effect is partially or fully dependent on histamine release processes. The substance is a competitive antagonist (with a powerful therapeutic effect) H1-terminations of histamine from the group of alkylamines. It has a minimal anticholinergic effect.

Pseudoephedrine with high efficiency eliminates swelling of the mucous in the upper part of the respiratory ducts, because it is a sympathomimetic with indirect and direct type of influence. In comparison with ephedrine, pseudoephedrine much less often leads to an increase in blood pressure and the development of tachycardia, and in addition, it does not stimulate the activity of the central nervous system so intensively.

[18], [19], [20], [21], [22], [23]

Pharmacokinetics

Pseudoephedrine triprolidine is well absorbed through the intestine in the case of oral use. After consuming 1 tablet, plasma Cmax values of triprolidine are approximately 5.5-6.0 ng / ml; the substance reaches these marks after 2 hours. Triprolidine half-life is about 3.2 hours. Only about 1% of the portion of triprolidine is excreted unchanged.

Pseudoephedrine Cmax values are approximately 180 ng / ml; it takes 120 minutes to reach them. Pseudoephedrine's half-life is 5.5 hours.

A 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 ration in an unchanged state. Pseudoephedrine excretion rates increase in the case of acidification of urine (respectively, they decrease with increasing urine pH level).

[24], [25], [26]

Dosing and administration

The patient should be warned that he needs to see a doctor if the signs of the disease do not go away after 7 days. It is required to follow medical instructions regarding the regimen and dosage size. It is forbidden to combine with other medicines that contain an antihistamine (among them, drugs for the treatment of cough and cold).

For adolescents from 12 years old and adults, a serving is 10 ml with 3-4 single intake per day. A maximum of 40 ml of the substance is allowed per day.

Children from the age group of 6-11 years require 3-4 times a day to use 5 ml of the medication. Per day is allowed to consume no more than 20 ml of Aktifed.

Children 2-6 years of age prescribed 2.5 ml of the drug 3-4 times a day. The maximum daily dose is 10 ml.

The sizes of portions of drugs for disorders in the work of the kidneys.

Pseudoephedrine is excreted through the kidneys. In case of insufficiency of renal activity, the plasma indicator of pseudoephedrine increases, therefore it cannot be used in people with insufficiency in the severe stage. Caution is required when appointing persons with moderate disruption.

Dosing regimen for disorders of hepatic activity.

Triprolidine is excreted mainly with the help of hepatic metabolic processes, which is why it is necessary to take into account the need to reduce the dosage for people with severe stages of hepatic disease.

[38], [39]

Use The effect during pregnancy

The drug should not be prescribed to breastfeeding mothers and pregnant women.

Contraindications

Main contraindications:

• the presence of intolerance against pseudoephedrine hydrochloride and triprolidine hydrochloride, and in addition to acrivastine or other auxiliary components of drugs;
• elevated blood pressure values (severe severity);
• CHD in severe stage;
• pheochromocytoma;
• failure of renal function in severe;
• severe renal or hepatic pathologies;
• bronchitis, BA or bronchiectasis, in which there is excessive secretion;
• use with other sympathomimetics (appetite suppressants, decongestants, and amphetamine-like psychostimulants);
• use in people who have taken or taken over the past 14 days of MAOI (this includes the antibacterial drug furazolidone).

[27], [28], [29], [30], [31], [32], [33],

Side effects The effect

Negative manifestations of pseudoephedrine.

Among the side effects:

• mental disorders: insomnia and nervousness are often noted. Sometimes there is anxiety, agitation, or tremor. Occasionally there are hallucinations (mainly in children);
• problems in NA: dizziness often appears. Sometimes headaches occur;
• lesions affecting the cardiovascular system: occasionally arrhythmia or tachycardia develops, the blood pressure level increases and the heartbeat increases. An increase in systolic blood pressure values was also recorded;
• disorders of the gastrointestinal tract: often nausea or vomiting, as well as dryness of the oral mucosa. Sometimes there is a deterioration in appetite;
• lesions of the subcutaneous layer and the epidermis: rarely there is hyperhidrosis, allergic dermatitis and rash. The use of pseudoephedrine can lead to the appearance of various signs of allergy from the epidermis (may be accompanied by systemic manifestations (angioedema and bronchospasm) or not);
• disorders affecting the urethra and the kidneys: urinary retention and dysuria are sometimes noted. Problems with urination occur mainly in people with obstruction of the urethra (for example, prostatic hypertrophy).

Negative symptoms of triprolidine.

Among the developing effects:

• mental disorders: paradoxical arousal is possible ((elderly people and children demonstrate the greatest sensitivity) feeling of anxiety or nervousness and increased energy), confusion (mostly observed in elderly people), delusions in a dream and hallucinations (usually in children);
• lesions affecting NA: often there is a feeling of drowsiness or a sedative effect. Also quite often recorded dizziness, inattention and disorder of coordination. Sometimes headaches occur;
• disorders of the cardiovascular system: sometimes there is tachycardia, orthostatic collapse and a feeling of weakness;
• manifestations on the part of the visual organs: the development of visual impairment is possible;
• lesions of the upper respiratory tract and organs of the sternum: possible nasal congestion and thickening of bronchial secretions;
• disorders in the gastrointestinal tract: often dry throat, as well as oral and nasal mucous membranes. You may experience discomfort in the gastrointestinal tract (vomiting with nausea), and in addition, obstruction, anorexia, heartburn or diarrhea, increased appetite and weight gain;
• disorders associated with the epidermis and the subcutaneous layer: photosensitivity, urticaria, or rash may occur;
• problems with the function of the urinary organs and kidneys: the occurrence of polyuria or dysuria, as well as urinary retention.

[34], [35], [36], [37]

Overdose

In case of poisoning with pseudoephedrine, signs may appear due to the stimulation of the activity of the cardiovascular system and the central nervous system (for example, anxiety or agitation, arrhythmia, hallucinations, vomiting, increased blood pressure, heart palpitations, nausea, dysuria and thirst). With severe overdose, convulsions, psychosis with hypertensive crisis, and comatose state appear.

Perhaps the decrease in serum potassium values - due to its transportation from the extracellular to the intracellular space.

Triprolidine intoxication is likely to provoke symptoms similar to the negative manifestations of this substance. In addition, there may be a feeling of weakness, tremor, ataxia, dryness of the mucous membranes and the epidermis, as well as the suppression of respiratory processes, psychosis, arrhythmia, hyperpyrexia, tachycardia and convulsions.

Required support activities are required to help eliminate the relevant specific features. Manifestations of CNS stimulation and convulsions are treated by parenteral injection of diazepam. The use of β-blockers eliminates hypokalemia and complications affecting the cardiovascular system.

[40], [41], [42], [43],

Interactions with other drugs

The combination of pseudoephedrine hydrochloride with an MAOI (or taking drugs for 14 days from the end of the course using an MAOI) can lead to the development of a hypertensive crisis. MAOI also potentiate the anticholinergic activity of triprolidine.

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

Reception together with sedative or hypnotic drugs, as well as tranquilizers potentiates the feeling of drowsiness. The same effect is observed when drinking alcohol during the use of drugs.

Pseudoephedrine can have an antagonistic effect if it is combined with certain antihypertensive drugs (for example, methyldopa, guanethidine with reserpine, as well as β-blockers and debrikosvin).

[44], [45], [46]

Storage conditions

Aktifed required to keep in a closed from small children, dark and dry place. Temperature values - not more than 25 ° С.

[47], [48], [49], [50], [51]

Shelf life

Aktifed can be used within 4 years from the moment of production of a therapeutic drug.

[52], [53], [54], [55], [56], [57], [58]

Application for children

Aktifed prohibited to use in children under 2 years of age.

[59], [60], [61], [62], [63], [64], [65], [66]

Analogs

Analogue of the drug is means Trifef.

[67], [68], [69], [70], [71], [72], [73]