Anesthetic suppository for hemorrhoids

Recommended local medications for the removal of pain symptoms of inflammation of the nodes formed in the anorectal area, primarily include an anesthetic suppository for hemorrhoids.

[1], [2], [3], [4], [5], [6], [7], [8], [9], [10], [11], [12]

Indications of the anesthetizing suppositories for hemorrhoids

Indications for the use of antihemorrhoidal drugs of this pharmacological group - a sense of pain in the anus, including during and after bowel movement.

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

[13], [14], [15], [16], [17]

Pharmacodynamics

Analgesic suppositories for hemorrhoids are applied topically and for the analgesic effect they have local anesthetics in their composition - substances that either reduce the sensitivity of painful afferent receptors of nerve fibers, or interfere with the transmission of painful nerve impulses.

Pharmacodynamics analgesic effect of suppositories Anestesol is based on the action of benzocaine, as well as menthol (whose content in one suppository is 25 times less than benzocaine). Benzocaine (synonymous with anesthesin) - ethyl ester of para-aminobenzoic acid - blocks the transmission of nerve signals by reducing the permeability of synaptic membranes for Na +. The localizing properties of menthol are less pronounced and are manifested by irritation of the nerve endings of the cold receptors of the rectal mucosa.

Anesthetic suppository for hemorrhoids Proctosan Neo, Proctogliolol and Doloproct have 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 NPVS buffeksamak, which blocks cyclooxygenase, reducing the synthesis of prostaglandins and the activity of neurotransmitters.

Analgesic effect of suppositories Anuzol, Betiol, as well as Suppositories with bellies is due to the content of the extract of the medicinal plant Atropa belladonna L (belladonna). Atropine alkaloid reduces the sensitivity of the cholinergic receptors of nerve endings, which causes a temporary disabling of local parasympathetic innervation in the area of rectal suppository application.

The localizing properties of the belladonna extract in the suppositories of Betiol are enhanced by ihtamol (ichthyol), which also reduces pain in hemorrhoids.

[18], [19], [20], [21]

Pharmacokinetics

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

Producers of Suppositories with bellies, Anuzol and Betiol pharmacokinetics of drugs have not been studied, since it is believed that with topical application, the belladonna extract does not cause systemic effects.

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

[22], [23], [24], [25]

Contraindications

Included in the review of analgesic suppository for hemorrhoids have the following contraindications to the use:

Anestezol - individual hypersensitivity to amide anesthetics, age to 18 years.

Anusol, Suppositories with belladonna, Betiol - prostatic 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 up to 14 years. The use of drugs with belladonna extract requires caution in the management of vehicles and mechanisms.

Proctosan Neo - atopic dermatitis, tuberculosis, syphilis, age under 18 years.

Proctoglivenol - individual sensitivity to components, age to 18 years.

Doloproct - shingles, tuberculosis, syphilis, children and adolescence.

Use of anesthetizing suppositories for hemorrhoids during pregnancy:

Anusole and Proctosan Neo are contraindicated.

Proctoglivenol and Doloproct are prohibited in the first trimester, in II and III are prescribed in cases where the expected benefit to the mother is higher than the potential risk to the fetus.

Anestezol, Suppositories with belladonna, Betiol - exclusively for the doctor's prescription, taking into account the likely risks for the unborn child.

[26], [27], [28], [29], [30]

Side effects of the anesthetizing suppositories for hemorrhoids

Manufacturers indicate side effects that can cause pain suppositories for hemorrhoids:

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

Anusolum, Suppositories with belladonna, Betiol - dry mouth, thirst, stools, urinary retention, urticaria, skin itching, headache, abdominal pain, increased heart rate, convulsions, temporary visual impairment, increased nervous excitement.

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

[31], [32], [33]

Dosing and administration

The only way to use an anesthetic suppository for hemorrhoids is rectal. It is recommended to enter the suppository into the rectum after defecation or cleansing enema.

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

Anesthetic suppository for hemorrhoids Proctosan Neo, Proctogliolol and Doloproct should be applied twice a day for one piece. You can not use Proctozan Neo for longer than a week, and the maximum duration of treatment for the suppository Doloproct is 14 days.

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

Overdose

In the instructions for the drugs Anestezol and Proctoglivenol, it is noted that "there have been no reports of an overdose of the drug, and the overdose of Proctozan Neo (for rectal administration) is not possible.

If some manufacturers of suppositories Anuzol claim that there is no data on drug overdose, then the instructions of other manufacturers state that overdose leads to an increase in the manifestations of adverse reactions (see earlier).

Symptoms of overdose Suppository with bellies and Betiol may be manifested by dysuria, a feeling of drying in the mouth and thirst, rapid heart rate, psychomotor agitation, etc.

Interactions with other drugs

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

Analgesic action of suppositories Anusolum decreases at simultaneous use of laxative preparations, means against a heartburn, preparations Metokloprom and Ketoconazole.

It is not recommended to apply Suppositories with bellies in combination with antihistamines, cardiothoric drugs based on digitalis (Digoxin, Digitoxin, Cordigit, etc.), beta-adrenostimulators, barbiturates and tricyclic antidepressants.

To avoid possible violations of the heart rhythm, analgesic suppository for hemorrhoids Doloproct is contraindicated to use if antiarrhythmic drugs are taken.

[38], [39], [40]

Storage conditions

All anesthetizing suppository 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 of not more than + 25 ° C.

[41], [42], [43], [44], [45], [46]

Shelf life

Shelf life of suppositories Anuzol, Betiol, Suppositories with belladonna, Doloproct is 2 years; Anestezol - 3 years; Proctozan Neo and Proctoglivenol - 5 years.

[47], [48], [49]