Analgesic suppositories for hemorrhoids

Local remedies recommended by doctors to relieve pain symptoms of inflammation of nodes formed in the anorectal area primarily include pain-relieving suppositories for hemorrhoids.

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Indications pain relieving suppositories for hemorrhoids.

Indications for the use of antihemorrhoidal drugs of this pharmacological group are the sensation of pain in the anus, including during and after bowel movements.

Among the most popular and effective means, it is necessary to note such names of pain-relieving suppositories for hemorrhoids as Anestezol, Anuzol (Neo-Anuzol), Suppositories with belladonna, Betiol, Proctozan Neo, Proctoglivenol, Doloproct.

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Pharmacodynamics

Pain-relieving suppositories for hemorrhoids are used locally and, to provide an analgesic effect, contain local anesthetics - substances that either reduce the sensitivity of pain afferent receptors of nerve fibers or prevent the transmission of pain nerve impulses.

The pharmacodynamics of the analgesic action of Anestezol suppositories is based on the action of benzocaine, as well as menthol (the content of which in one suppository is 25 times less than benzocaine). Benzocaine (a synonym for anesthesin) is an ethyl ester of para-aminobenzoic acid that blocks the transmission of nerve signals by reducing the permeability of synaptic membranes for Na+. The local anesthetic properties of menthol are less pronounced and are manifested by irritation of the nerve endings of the cold receptors of the rectal mucosa.

Pain-relieving suppositories for hemorrhoids Proctozan Neo, Proctoglivenol and Doloproct contain lidocaine in the form of hydrochloride (α-diethylamino-2,6-dimethylacetanilide hydrochloride), which acts in the same way as benzocaine. In addition, Proctozan Neo suppositories contain the NSAID bufexamak, which blocks cyclooxygenase, reducing the synthesis of prostaglandins and the activity of neurotransmitters.

The analgesic effect of Anuzol, Betiol suppositories, as well as belladonna suppositories is due to the content of the extract of the medicinal plant Atropa belladonna L (belladonna). The belladonna alkaloid atropine reduces the sensitivity of the cholinergic receptors of the nerve endings, which causes a temporary shutdown of local parasympathetic innervation in the area of application of rectal suppositories.

The local anesthetic properties of belladonna extract in Betiol suppositories are enhanced by ichthammol (ichthyol), which also reduces pain in hemorrhoids.

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Pharmacokinetics

According to the official instructions, the pharmacokinetics of the drug Anestezol have not been studied, although it is known that benzocaine, which is part of these suppositories, acts quickly, but not for long, is weakly absorbed into the mucous membranes, but, nevertheless, is found in the blood plasma. Benzocaine partially destroys in the blood, the rest - in the liver, and the metabolic products are excreted from the body by the kidneys.

The manufacturers of Belladonna Suppositories, Anuzol and Betiol have not studied the pharmacokinetics of the drugs, since it is believed that when applied locally, belladonna extract does not cause systemic effects.

Lidocaine, which is contained in the analgesic suppositories for hemorrhoids Proctozan Neo, Proctoglivenol and Doloproct, according to the instructions for these products, is absorbed by 24%, and its highest concentration in plasma is noted two hours after the use of suppositories. Biotransformation of lidocaine occurs in the liver (by hydroxylation), metabolites (4-hydroxy-2,6-xylidine) are excreted in the urine.

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Dosing and administration

The only way to use pain-relieving suppositories for hemorrhoids is rectal. It is recommended to insert the suppository into the rectum after defecation or a cleansing enema.

Anestezol is administered one suppository 1-2 times a day. Anuzol, Belladonna suppositories, Betiol - one suppository 2-3 times a day; the maximum daily dose of Anuzol is 7 suppositories, Belladonna suppositories and Betiol - 10.

Pain-relieving suppositories for hemorrhoids Proctozan Neo, Proctoglivenol and Doloproct should be used twice a day, one at a time. Proctozan Neo should not be used for longer than a week, and the maximum duration of treatment with Doloproct suppositories is 14 days.

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Contraindications

The analgesic suppositories for hemorrhoids included in the review have the following contraindications for use:

Anestezol – individual hypersensitivity to amide anesthetics, age under 18 years.

Anuzol, Belladonna suppositories, Betiol - prostate adenoma, dysuria, thyrotoxicosis, chronic heart failure, ischemic heart disease, atrial fibrillation and tachycardia, hypertension, intestinal atony, progressive autoimmune muscle weakness (myasthenia gravis), acute bleeding, glaucoma, age under 14 years. The use of drugs with belladonna extract requires caution when driving vehicles and operating machinery.

Proctozan Neo – atopic dermatitis, tuberculosis, syphilis, age under 18 years.

Proctoglivenol – individual sensitivity to components, age under 18 years.

Doloproct - herpes zoster, tuberculosis, syphilis, childhood and adolescence.

Using pain-relieving suppositories for hemorrhoids during pregnancy:

Anuzol and Proctozan Neo are contraindicated.

Proctoglivenol and Doloproct are prohibited in the first trimester; in the second and third trimesters they are prescribed in cases where the expected benefit to the mother is higher than the potential risk to the fetus.

Anestezol, Belladonna suppositories, Betiol - only as prescribed by a doctor, taking into account the possible risks to the unborn child.

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Side effects pain relieving suppositories for hemorrhoids.

Manufacturers indicate side effects that can be caused by pain-relieving suppositories for hemorrhoids:

Anestezol – skin rash, itching, hives, burning in the anus, problems with stool, blood composition disorders (with prolonged use).

Anuzol, Belladonna suppositories, Betiol - dry mouth, thirst, bowel disturbances, urinary retention, urticaria, itchy skin, headache, abdominal pain, increased heart rate, convulsions, temporary deterioration of vision, increased nervous excitement.

Proctozan Neo, Proctoglivenol and Doloproct – skin rash and itching, burning in the anorectal area.

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Overdose

The instructions included with the drugs Anestezol and Proctoglivenol state that “there have been no reports of drug overdose, and an overdose of Proctozan Neo (with rectal use) is impossible.

While some manufacturers of Anuzol suppositories claim that there is no data on drug overdose, the instructions from other manufacturers indicate that overdose leads to increased manifestations of side effects (see above).

Signs of an overdose of Belladonna and Betiol suppositories may include dysuria, a feeling of dry mouth and thirst, increased heart rate, psychomotor agitation, etc.

Interactions with other drugs

Pharmacologically significant interactions with other drugs of Anestezol, Betiol, Proctozan Neo and Proctoglivenol suppositories are not indicated in the instructions.

The analgesic effect of Anuzol suppositories is reduced with the simultaneous use of laxatives, heartburn medications, Metocloprom and Ketoconazole.

It is not recommended to use Belladonna suppositories in combination with antihistamines, cardiotonic drugs based on digitalis (Digoxin, Digitoxin, Cordigit, etc.), beta-adrenergic stimulants, barbiturates and tricyclic antidepressants.

To avoid possible disturbances in heart rhythm, pain-relieving suppositories for hemorrhoids Doloproct are contraindicated if antiarrhythmic drugs are taken.

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Storage conditions

All pain-relieving suppositories for hemorrhoids should be stored in a place protected from light; Anestezol, Anuzol and Betiol - at a temperature of +10-15°C; Suppositories with belladonna, Proctozan Neo, Proctoglivenol and Doloproct - at a temperature not exceeding +25°C.

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Shelf life

The shelf life of Anuzol, Betiol, Belladonna suppositories, Doloproct is 2 years; Anestezol – 3 years; Proctozan Neo and Proctoglivenol – 5 years.

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