Amitriptyline

Trade name:
Damilena maleinat

The international name:
Amitriptyline (Amitriptyline)

Group Affiliation:
Antidepressant

Description of the active substance (INN):
Amitriptyline

Dosage form:
tablets, capsules, solution for intramuscular injection, tablets, coated tablets

Mode of action:
Antidepressant drug (tricyclic antidepressant). Also has some analgesic (of central genesis), H2-gistaminoblokiruyuschee and antiserotoninovoe action helps eliminate bed-wetting and reduces appetite. Possesses a strong peripheral and central anticholinergic effects associated with high affinity to the m-cholinergic receptors, a strong sedative effect connected with affinity for H1 -histamine receptors, and alpha-adrenoceptor blocking action. Has the properties of anti-arrhythmic drugs subgroups Ia, like quinidine at therapeutic doses slows ventricular conduction (in overdose can cause severe intraventricular block). The mechanism of antidepressant action is associated with an increase in the concentration of noradrenaline in the synapses and / or serotonin in the central nervous system (reduction of the reverse suction). The accumulation of these neurotransmitters is the result of inhibition of return of their capture membranes of presynaptic neurons. Prolonged use reduces the functional activity of beta-adrenergic and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems are impaired in depressive states. When anxiety and depressive states reduces anxiety, agitation and depressive manifestations. Antiulcer mechanism of action is due to the ability to block histamine H2-receptors in parietal cells of the stomach, as well as to provide sedative and anticholinergic effects of m-(for stomach ulcers and 12 duodenal ulcer reduces the pain, accelerates healing of ulcers). Efficiency at bed-wetting is due, apparently, anticholinergic activity, which leads to an increase in the ability of the bladder to stretch, direct beta-adrenergic stimulation, the activity of alpha-adrenergic agonists, accompanied by increased tone of sphincter and the central blockade of seizure serotonin. have a central analgesic action, which is believed to be associated with changes in concentrations of monoamines in the CNS, especially serotonin, and the impact on the endogenous opioid system. The mechanism of action for bulimia nervosa is unclear (perhaps similar to those for depression). Showed a distinct effect of the drug in patients with bulimia as no depression, and if available, to the reduction of bulimia may occur without a concomitant weakening of the depression itself. In the conduct of general anesthesia, reduces blood pressure and body temperature. Did not inhibit MAO. Antidepressive action develops within 2-3 weeks after application.

Indications:
Depression (especially with anxiety, agitation and sleep disorders, including childhood, endogenous, involutional, reactive, neurotic, drug, with organic brain damage, alcohol withdrawal), schizophrenic psychoses, mixed emotional disturbances, disturbances in behavior (Activity and attention), nocturnal enuresis (except in patients with hypotonia of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical facial pain, postherpetic neuralgia, posttraumatic neuropathy, diabetic or other peripheral neuropathy), headaches, migraine (prevention), peptic ulcer and 12 duodenal ulcer.

Contraindications:
Hypersensitivity, used in conjunction with MAO inhibitors and for 2 weeks before starting treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotics, analgesic and psychoactive drugs, angle-closure glaucoma, severe violations of AV and intraventricular conduction (block feet beam branch block, AV block II cent.), lactation period, children's age (up to 6 years - oral forms, up to 12 years with the / m and / in the introduction). C care. Chronic alcoholism, asthma, manic-depressive psychosis, depression of bone marrow hematopoietic diseases, CAS (angina, arrhythmias, heart block, CHF, myocardial infarction, hypertension), stroke, reduced motor function of the gastrointestinal tract (risk of paralytic ileus), intraocular hypertension , liver and / or renal failure, hyperthyroidism, prostatic hyperplasia, urinary retention, hypotension bladder, schizophrenia (possible activation of psychosis), epilepsy, pregnancy (especially the I term), advanced age.

Adverse effects:
Anticholinergic effects: blurred vision, cycloplegia, mydriasis, increased intraocular pressure (only persons with local anatomical predisposition - a narrow angle of anterior chamber), tachycardia, dry mouth, confusion, delirium or hallucination, constipation, paralytic ileus, difficulty urinating , reduction of perspiration. the nervous system: drowsiness, asthenia, fainting, anxiety, disorientation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, agitation, restlessness, manic state, hypomanic state, aggressiveness, memory impairment, depersonalization, increased depression, reduced ability to concentrate, insomnia, nightmares, dreams, yawning, asthenia, activation of the symptoms of psychosis, headache, myoclonus, dysarthria, tremor of small muscles, especially the hands, arms, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, quickening and strengthening of epileptic seizures, EEG changes. On the part of the SSA: tachycardia, palpitations, dizziness, orthostatic hypotension, nonspecific ECG changes (ST interval and T wave) in patients not suffering from heart disease; arrhythmia, blood pressure lability (decreased or increased blood pressure), violation of intraventricular conduction (increasing complex QRS, change the interval PQ, bundle branch block feet). On the part of the digestive system: nausea, rarely - hepatitis (including dysfunction liver and cholestatic jaundice), indigestion, vomiting, stomachalgia, increased appetite and body weight, or decreased appetite and weight, sores, taste changes, diarrhea, darkening of the tongue. On the part of the endocrine system: an increase in size (swelling) of testicles, gynecomastia, an increase the size of breasts, galactorrhea, decreased or increased libido, reduced potency, hypo-or hyperglycemia, hyponatremia (decreased production of vasopressin), a syndrome of inappropriate secretion of ADH. From the side of hematopoiesis: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia. Allergic reactions: skin rash, itching, skin rash, photosensitization, edema of the face and tongue. Other: Hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urine retention, thamuria, hypoproteinemia. withdrawal symptoms: the sudden cancellation after long-term care - nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual excitement, with the gradual abolition after long-term care - irritability, restlessness, sleep disturbances, unusual dreams. Communication with the drug intake is not installed: volchanochnopodobny syndrome (migratory arthritis, the appearance of antinuclear antibody and positive rheumatoid factor), abnormal liver function, ageusia. Local reaction to the in / in the introduction: thrombophlebitis, lymphangitis, burning sensation, allergic skin reaktsii.Peredozirovka. Symptoms. On the part of the CNS: drowsiness, stupor, coma, ataxia, hallucinations, anxiety, psychomotor agitation, reduced ability to concentrate, disorientation, confusion, dysarthria, hyperreflexia, muscular rigidity, choreoathetosis, epileptic syndrome. On the part of the SSA: BP decrease, tachycardia , arrhythmia, a violation of intracardiac conduction, characteristic of tricyclic antidepressants intoxication, ECG changes (especially the QRS), shock, CH, in very rare cases - cardiac arrest. Other: respiratory depression, apnea, cyanosis, vomiting, hyperthermia, mydriasis, increased sweating, oliguria or anuria. The symptoms develop within 4 h after the overdose, reach a maximum after 24 h and lasts 4-6 days. If you suspect an overdose, especially in children, the patient should be hospitalized. Treatment: Ingestion: gastric lavage, the appointment of activated charcoal, symptomatic and supportive therapy, in severe anticholinergic effects (lowering of blood pressure, arrhythmias, coma, myoclonic epileptic seizures) - the introduction of inhibitors cholinesterase (application Physostigmine is not recommended because of the increased risk of convulsions); maintenance of blood pressure and water and electrolyte balance. Showing the control functions of SSA (including ECG) within 5 days (relapse can occur after 48 h and later), anticonvulsant therapy, mechanical ventilation and other resuscitation. Hemodialysis and forced diuresis are ineffective.

Dosage and administration:
Inside, not liquid, immediately after a meal (to reduce the irritation of the mucous membrane of the stomach). The initial dose for adults - 25-50 mg at night, then increase the dose for 5-6 days to 150-200 mg / day in 3 divided doses (maximum dose is taken on the part of the night). If within 2 weeks of no improvement occurred, the daily dose increased to 300 mg. With the disappearance of signs of depression reduce the dose to 50-100 mg / day and continue treatment at least 3 months. In old age with lung disorders prescribed in doses of 30-100 mg / day (at night), after reaching the therapeutic effect of switching to the minimum effective dose - 25-50 mg / day. V / m or / to (enter slowly) in a dose 20-40 mg 4 times a day, gradually replacing ingestion. Duration of treatment - no more than 6-8 months. In nocturnal enuresis in children 6-10 years - 10-20 mg / day for the night, 11-16 years - 25-50 mg / day. Children as an antidepressant: 6 to 12 years - 10-30 mg or 1-5 mg / kg / d fractional, in adolescence - 10 mg 3 times a day (if necessary, up to 100 mg / day). For the prevention of migraine, chronic pain neurogenic nature (in m . hour long headaches) - from 12.5-25 to 100 mg / day (maximum dose taken part in the night).

Cautions:
Before treatment is necessary to monitor blood pressure (in patients with low or labile blood pressure, it can be reduced even more) during treatment - control peripheral blood (in some cases may develop agranulocytosis, and therefore it is recommended to monitor blood picture, especially when increase in body temperature, the development of influenza-like symptoms and sore throat), with long-term therapy - control functions of the SSA and the liver. In elderly and patients with diseases of the SSA shows control of heart rate, blood pressure, ECG. The ECG may result in clinically insignificant changes (smoothing of the T wave, depression of segment ST, the expansion of the complex QRS). Parenteral use is possible only in hospital under medical supervision, compliance with bed rest in the first days of therapy. Caution is necessary when a dramatic shift in the vertical position from the "lying" or "sitting." During the period of treatment should eliminate the use of ethanol. Assign no earlier than 14 days after discontinuation of MAO inhibitors, beginning with small doses. At the reception following the sudden cessation of long-term treatment may develop the syndrome of "cancel." Amitriptyline at doses above 150 mg / day lowers the threshold for seizure activity (it should take into account the risk of epileptic seizures in susceptible patients, as well as the presence of other predisposing factors, the emergence of cramps, such as traumatic brain injury of any etiology, the simultaneous use of antipsychotic drugs (neuroleptics) during the period of non-ethanol or cancellation of drugs with anticonvulsant properties, such as benzodiazepines). pronounced depression of the peculiar risk of suicidal actions, which may persist until a substantial remission. In this regard, early treatment may be in combination with the drug from the group of benzodiazepines, or antipsychotic drugs and constant medical control (charging proxies storage and issuing of drugs). In patients with cyclic affective disorders during the depressive phase of the therapy may develop manic or hypomanic (requires dose reduction or withdrawal of the drug and the appointment of antipsychotic drugs). After coping with these states, if there are indications, treatment at low doses may be renewed. Because of the possible effects of cardiotoxicity requires careful when treating patients with thyrotoxicosis or patients receiving thyroid hormone drugs. In conjunction with electroconvulsive therapy shall be appointed only with careful medical supervision . In predisposed patients and elderly patients may result in the development of drug psychoses, mainly at night (after the withdrawal of the drug are within a few days). It can cause paralytic ileus, mainly in patients with chronic constipation, elderly, or patients who are forced to comply bed rest. Prior to the general or local anesthesia should alert the anesthesiologist that the patient is taking amitriptyline. Because anticholinergic actions may reduce watery, and the relative increase in mucus in the tear fluid, which can cause damage to the corneal epithelium in patients who use contact lenses. Prolonged use of an increase in the incidence of dental caries. Can be increased need for riboflavin. The study of reproduction in animals showed adverse effects on the fetus, and adequate and strictly controlled studies in pregnant women has not held. Pregnant women should use the drug only if the intended benefits to the mother outweighs the potential risk to the fetus. Penetrates into breast milk and may cause drowsiness in infants. In order to avoid the development of the syndrome of "cancellation" in neonates (manifested wheezing, drowsiness, intestinal colic, increased nervous excitability, hypotension or hypertension, tremor or spastic phenomena) receiving amitriptyline gradually canceled at least 7 weeks prior to delivery. Children are more susceptible to acute overdosage, which should be considered dangerous and potentially fatal for them. In the period of treatment to be careful when driving vehicles and other lesson potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Interaction:
When the joint application of ethanol and drugs which depress the central nervous system (including other antidepressants, barbiturates, and general anesthetics benzadiazepinov), possibly a considerable increase in inhibitory action on CNS, respiratory depression and hypotensive effect. Increases the sensitivity to drinks containing ethanol. Increases anticholinergic effects of drugs with anticholinergic activity (eg phenothiazines, antiparkinsonian drugs, amantadine, atropine, biperidena, antihistamine drugs), which increases the risk of side effects (from the central nervous system, eyes, intestines and bladder). When combined with the use of antihistamine drugs, clonidine - strengthening of inhibitory action on CNS, with atropine - increases the risk of paralytic ileus, with drugs causing extrapyramidal reactions - the severity and frequency of extrapyramidal effects. With simultaneous application of amitriptyline, and indirect anticoagulants (coumarin derivatives or indadiona) may increase anticoagulant activity of the past . Amitriptyline may increase the depression caused by SCS. When combined with the use of anticonvulsant drugs may be increased inhibitory action on the central nervous system, reducing the threshold for seizure activity (when used in high doses) and reduced the effectiveness of the latter. drugs for the treatment of thyrotoxicosis increase the risk of agranulocytosis. reduces the effectiveness of phenytoin and alpha-blockers. microsomal oxidation inhibitors (cimetidine), extend T1 / 2, increase the risk of toxic effects of amitriptyline (may require dose reduction of 20-30%), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine, oral contraceptives) reduce the concentration in plasma and reduce the effectiveness of amitriptyline. Fluoxetine and fluvoxamine increase the concentration of amitriptyline in plasma (may require reducing the dose of amitriptyline to 50%). In a joint application with holinoblokatorami, phenothiazines and benzodiazepines - are mutually reinforcing sedative and central anticholinergic effects and increased risk of epileptic seizures (threshold decrease seizure activity), phenothiazines, in addition, may increase the risk of neuroleptic malignant syndrome. In case of simultaneous application of amitriptiliina with clonidine guanetidinom, betanidinom, reserpine and methyldopa - decrease the hypotensive effect of the latter; with cocaine - the risk of cardiac arrhythmias. Estrogensoderzhaschie Oral contraceptive drugs and estrogens may increase the bioavailability of amitriptyline; antiarrhythmic drugs (like quinidine) increase the risk of arrhythmias (possibly slow metabolism of amitriptyline). The combined use of disulfiram and other inhibitors atsetaldegidrogenazy provoke delirium. incompatible with MAO inhibitors (possible increase in the frequency of periods hyperpyrexia , severe convulsions, hypertensive crises, and the patient's death). Pimozid and probucol may increase cardiac arrhythmia, which is manifested by the lengthening of the QT interval on ECG. intensifies the effect of the SCA epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine (including if when these drugs are part of local anesthetics), and increases the risk of cardiac arrhythmia, tachycardia, severe hypertension. In a joint appointment with the alpha-adrenostimulyatorov for intranasal administration, or for use in ophthalmology (with significant systemic absorption) can increase the vasoconstrictor action of the latter. In a joint reception with thyroid hormones - the mutual reinforcement of therapeutic effects and toxic effects (including cardiac arrhythmia and a stimulating effect on CNS). M-holinoblokatory and antipsychotic drugs (neuroleptics) increase the risk of hyperpyrexia (especially during hot weather). At a joint appointment with etc. gematotoksichnymi drugs may gain gematotoksichnosti.

Trypsin

Trade name:
Daltseks-Trypsin

The international name:
Trypsin (Trypsin)

Group Affiliation:
Proteolytic topica

Description of the active substance (INN):
Trypsin

Dosage form:
lyophilisates for solution for injection and local application, lyophilisates for solution for local and external use, napkin treatments

Mode of action:
Endogenous proteolytic enzymes. Optimum action - at pH 7-9. When applied topically has anti-inflammatory, Burns, recycling and nekroliticheskoe action. Cleaves the necrotic tissue and fibrous education, promotes rejection of necrotic tissue liquefies pus and facilitates its separation, improves the process of regeneration of wounds. There is no change in the hemostatic system. In relation to the healthy tissue is inactive and is safe in relation to the presence of trypsin inhibitors (specific and nonspecific).

Indications:
Diseases of the respiratory tract, pleural empyema, pleural effusion, thrombophlebitis, periodontitis (inflammatory-dystrophic form), osteomyelitis, sinusitis, otitis media, iritis, iridocyclitis, hemorrhage into the anterior chamber of the eye, edema periorbital area after operations and injuries, burns, pressure sores, festering wounds (used topically).

Contraindications:
Hypersensitivity, decompensated chronic heart failure, pulmonary emphysema with respiratory insufficiency, and decompensated forms of pulmonary tuberculosis, liver, liver cirrhosis, pancreatitis, infectious hepatitis, hemorrhagic diathesis. You can not enter into the cavity bleeding, I / O and applied on the surface of ulcerated tumors.

Adverse effects:
Allergic reactions, hyperthermia, tachycardia. When i / m administration - pain, congestion at the injection site, when inhaled - irritation of the mucous membranes of the upper respiratory tract, hoarseness.

Dosage and administration:
V / m: adults - 5-10 mg 1-2 times a day for children - to 2.5 mg 1 time a day. For injection immediately before use diluted 5 mg of crystalline trypsin in 2.1 ml 0.9% NaCl solution or 0.5-2% solution of procaine. The treatment course - 6-15 injections. Applied also electrophoresis with trypsin: 1 procedure 10 mg of trypsin (dissolved in 15-20 ml of distilled water), injected with the negative pole. Inhaler: 5-10 mg in 2-3 ml 0.9% NaCl solution through a nebulizer or a bronchoscope. After inhalation rinse your mouth with warm water and washed his nose. Eye drops: 0.2-0.25% solution, which is prepared immediately before use. Intraplevralno: 1 time per day, 10-20 mg, dissolved in 20-50 ml 0.9% solution of NaCl. Locally: in the form of powder or a solution of trypsin amorphous, dry or necrotic wounds impose compresses (a solution prepared immediately before use: 50 mg of trypsin dissolved in 5 ml of sterile water or 0.9% solution of NaCl, in the treatment of purulent wounds - in 5 ml phosphate buffer). Intraplevralno: 50-150 mg for in 5-30 ml phosphate buffer solution, preferably after the introduction of frequent changes in body position, on day 2 after instillation released, usually attenuated exudate. Triple woven cloth from dialdegidtsellyulozy, soaked in trypsin, impose on the wound (after treatment) and fixed with bandage on the wound, leaving no more than 24 hours before using cloth moistened with distilled water or solution furacilinum. Time of complete cleansing wounds of necrotic tissue and pus - 24-72 h. If necessary, apply again.

DALFUSINUM

Pharmacological properties: antidizuricheskoe tool. Selectively blocking postsynaptic α 1-adrenergic receptors located in the triangle of the bladder, urethra and prostate gland, prevents spasm of sphincters of the bladder, urethra and prostate gland, reduces vnutriuretralnoe pressure. It improves urodynamic parameters: lowering the tone of the urethra and the resistance of the outflow from the bladder facilitates the process of emptying, significantly increases the maximum rate of urine outflow, reduces residual urine volume, causing a strong urge to urinate due to increased volume of urine.

Well absorbed in the gastrointestinal tract. The maximum plasma concentration achieved after 3 h. The binding with plasma proteins is about 90%. The half alfuzozina - 8 pm Only 11% alfuzozina excreted unchanged in the urine. Metabolised in the liver, the majority of inactive metabolites (75-91%) is excreted in the feces.

Elderly patients noted a higher plasma concentration and bioavailability (possibly by reducing the metabolism in the liver), volume of distribution decreases, half-life remains unchanged. In patients with renal insufficiency volume of distribution increases, and the total clearance alfuzozina increases (perhaps by reducing the binding to plasma proteins). Even in the case of severe renal insufficiency not cumulative due to intense biotransformation. In chronic heart failure pharmacokinetic parameters are not changed.

INDICATIONS: Symptomatic treatment of benign prostatic hyperplasia.

APPLICATION: designate an adult male inside after eating without chewing 1 tablet (5 mg) morning and evening. Elderly patients and patients with renal failure and / or patients receiving antihypertensive therapy, prescribed 1 tablet in the evening, and if necessary increase the dose to 2 tablets (morning and evening).

The maximum daily dose - 2 tablets (10 mg).

CONTRAINDICATIONS: Hypersensitivity to any component of the drug, orthostatic hypotension, simultaneous reception of other α 1-blockers, hepatic failure.

SIDE EFFECTS:

From the CNS: headache, dizziness, tinnitus, weakness, seldom - syncope, asthenia, somnolence.

Since the cardiovascular system: rarely - orthostatic hypotension, palpitation, tachycardia, aggravation of symptoms of angina (in patients with coronary heart disease), pain in the chest, edema, flushing.

On the part of the digestive system: nausea, diarrhea, pain in the epigastric region, rarely - dry mouth.

Other: rarely - skin rash, itching.

Cautions: Patients with coronary heart disease, hypertension, renal failure receiving antihypertensive therapy, dosage adjustment is necessary. If during therapy the worsening angina pectoris, the drug should be abolished. The drug can be prescribed as in AH, and at a normal level of blood pressure, in the latter case, blood pressure reduction is not significant.

Because while taking the drug may develop hypotension and dizziness, is not recommended to drive vehicles or to perform work that requires increased attention.

Not intended for use in women and children.

INTERACTION: incompatible with other blockers, α 1-adrenoceptor. The drug potentiates the effects of antihypertensive agents and general anesthetics (possible instability BP).

OVERDOSE:

Symptoms: hypotension. The patient must be in the supine position.

Treatment: symptomatic - Introduction vasoconstrictor agent, p-ditch high molecular substances that increase the BCC. Hemodialysis is ineffective.

Storage: Store in dark place at a temperature of 25 ° C.

Alfuzosin

Trade name:
Dalfaz

The international name:
Alfuzozin (Alfuzosin)

Group Affiliation:
Alpha 1-blocker

Description of the active substance (INN):
Alfuzozin

Dosage form:
coated tablets, tablets with prolonged action, prolonged action tablets coated

Mode of action:
Alpha 1-adrenoceptor blocker (mainly in the zone of the prostate, urethra and bladder of the triangle). Reduces pressure in the urethra and reduces resistance to the current urine facilitates urination and eliminates dysuria, including with prostatic hyperplasia. In therapeutic doses has no effect on alpha 1-adrenergic receptors of the vessels.

Indications:
Functional urination disorders in benign prostatic hyperplasia.

Contraindications:
Hypersensitivity, orthostatic hypotension (history), simultaneous reception of other alpha-adrenoblokatorov.C caution. Coronary heart disease, chronic renal failure, concomitant therapy antihypertensive drugs, advanced age (older than 75 years).

Adverse effects:
On the part of the digestive system: dry mouth, nausea, pain in the epigastrium, diarrhea. On the part of the nervous system: headache, dizziness, weakness, drowsiness, asthenia syndrome with SSS by: tachycardia, orthostatic hypotension, in patients with coronary heart disease - exacerbation of symptoms of angina. Allergic reactions: skin rash, itching. Other: tinnitus, edema, hyperemia kozhi.Peredozirovka. Symptoms: blood pressure reduction. Treatment: Introduction vasoconstrictive means, solutions of high molecular substances, the increase in BCC, dialysis - is ineffective.

Dosage and administration:
Inside, not liquid, 5 mg in the morning and evening, begin treatment with an evening reception. Daily dose - 10 mg. Elderly or patients receiving antihypertensive therapy, prescribed at 5 mg / day, at night, if necessary, dose increased to 10 mg / day (no more).

Interaction:
Not compatible with other alpha1-blockers. Strengthens effect of antihypertensive drugs, including BCCI and general anesthetics (possible unstable blood pressure during anesthesia)

DALTEPARIN SODIUM

Pharmacological action

Anticoagulant of direct action. It is a low molecular weight heparin (average molecular weight of 4000-6000 daltons), isolated from the mucosa of the small intestine of pig. Binds antithrombin plasma, as a consequence is the suppression of some clotting factors, primarily, a factor Xa; significantly inhibited the formation of thrombin. Renders poorly marked effect on the adhesion of platelets. Slightly increases the APTT and thrombin time.


Pharmacokinetics

Pharmacokinetic parameters of dalteparin sodium did not vary according to the administered dose. After sc injection of bioavailability is about 90%.

T 1 / 2 after i / v injection of 2 h, after s / c - 3-4 hours is derived mainly by the kidneys.

In patients with severe impaired renal function T 1 / 2 increases.


Statement

Acute deep vein thrombosis, prevention of blood clotting in the extracorporeal circulation during long-term hemodialysis or hemofiltration in patients with acute or chronic renal failure, prevention of thromboembolic complications in pre-and postoperative period; unstable angina or myocardial infarction (without pathological tooth Q).


Dosage regimen

Dose was set individually, depending on indications, clinical situation and applied treatment regimens. Enter in / jet or drip, and n / k.

Not intended for the / m injection.


Side effect

On the part of the hemopoietic system and blood coagulation system: rarely - thrombocytopenia, bleeding (when used in high doses).

On the part of the digestive system: in some cases - increase in liver transaminases.

Local reactions: the formation of subcutaneous hematoma at the injection site, rarely - necrosis of the skin.


Contraindications

Serious breaches of the blood coagulation system, stomach ulcer and duodenal ulcer in acute, bacterial endocarditis, trauma central nervous system, organs of vision, hearing, and oral surgery on these organs, the simultaneous application of local anesthesia (for the treatment of acute deep vein thrombosis) and unstable angina, increased sensitivity to dalteparin sodium.


Application of pregnancy and breastfeeding

There are no adequate and strictly controlled studies of safety during pregnancy and lactation (breastfeeding) was carried out. A small clinical experience with dalteparin sodium during pregnancy indicates the absence of any negative effect on pregnancy and child health.

Unknown is allocated whether dalteparin sodium in breast milk.


Cautions

With careful use dalteparin sodium in patients with thrombocytopenia or platelet defects, marked disturbances of liver function, uncontrolled hypertension, hypertensive or diabetic retinopathy, with hypersensitivity to heparin or low molecular weight heparin in history; patients in the early postoperative period.

Increasing doses of dalteparin sodium in order to increase the APTT may lead to overdose and bleeding. For laboratory monitoring of treatment dalteparin sodium should use tests to determine anti-Xa activity.

In an emergency hemodialysis requires a more careful control of the activity level of anti-Xa because of the narrow range of therapeutic doses for these patients.

In patients with transmural myocardial infarction, developed in the presence of unstable angina and myocardial infarction without pathological Q wave in the case of thrombolytic therapy cancellation dalteparin sodium is optional. However, in such a situation increases the risk of bleeding.


Drug Interactions

With the simultaneous use of antihistamines, cardiac glycosides, tetracycline, ascorbic acid reduced the effectiveness of dalteparin sodium.

With the simultaneous use of NSAIDs, antagonists of vitamin K, dipyridamole, dextran, sulfinpirazon, probenecid, ethacrynic acid, cytotoxic drugs (for i / v injection) increases the effects of dalteparin sodium.

Flurazepam

Trade name:
Dalmadorm

The international name:
Flurazepam (Flurazepam)

Group Affiliation:
Soporific

Description of the active substance (INN):
Flurazepam

Mode of action:
Hypnotic benzodiazepine. Also has anxiolytic, anticonvulsant and central miorelaksiruyuschee action. Assign usually as a sedative-hypnotics drugs. Strengthens the inhibitory effect of GABA (neurotransmitter pre-and postsynaptic inhibition in all parts of the CNS) to the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating brain stem reticular formation and lateral horn neurons of the spinal cord, reduces the excitability of the subcortical brain structures (limbic system, thalamus, hypothalamus), inhibits the polysynaptic spinal reflexes. Anxiolytic effects due to the influence on the amygdaloid complex of the limbic system and appears to reduce the emotional stress, reducing anxiety, fear, anxiety. Sedation due to the influence on the reticular formation of the brain stem and nonspecific thalamic nucleus and manifests a decrease in symptoms of neurotic origin (anxiety, fear). The main mechanism of action is soporific in the inhibition of cells of the reticular formation of the brain. Reduces the impact of emotional, autonomic and motor stimuli that violate the mechanism of sleep. Reduces the duration of the period of sleep, reduces the number of awakenings, increase sleep. Therapeutically significant effect occurs at 2-3 overnight after starting treatment. Anticonvulsant action is realized by increasing presynaptic inhibition. Reduces spread of epileptogenic activity, but not removed the excited state of the hearth. Miorelaksiruyuschee central action is caused by inhibition of spinal polysynaptic afferent inhibitory ways (to a lesser extent and monosynaptic). It is possible, and direct inhibition of motor nerve and muscle function. The productive psychotic symptoms genesis (acute delusional, hallucinatory, affective disorders) has practically no effect, is rarely observed decrease in affective intensity, delusional disorders.

Indications:
Sleep disorders: a violation of falling asleep, nocturnal awakening, early awakening.

Contraindications:
Hypersensitivity, coma, shock, acute alcohol intoxication with a weakening of the vital functions, acute intoxication of drugs, have a depressing effect on the central nervous system (including narcotic analgesics and hypnotics drugs), myasthenia gravis, angle-closure glaucoma (acute onset or predisposition), severe COPD (degree of progression of respiratory failure), acute respiratory failure, paradoxical reactions to ethanol and / or sedative drugs, severe depression (suicidal tendencies may be observed), pregnancy (especially the I trimester), lactation, age 15 (safety and efficacy have not identified ). C care. Depression, liver and / or renal failure, cerebral and spinal ataxia, hyperkinesis, drug dependency history, the propensity to abuse drugs, organic brain disease, psychosis (possible paradoxical reactions), hypoproteinemia, respiratory disorders due to depression of the respiratory center (in including sleep apnea, established or suspected), advanced age.

Adverse effects:
Of the nervous system: at the beginning of treatment (particularly in older patients) - drowsiness, fatigue, dizziness, reduced ability to concentrate, ataxia, unsteady gait and poor coordination of movements, apathy, blunting of emotions, mental retardation and motor responses, seldom - headache, euphoria, depression, tremor, depressed mood, catalepsy, anterograde amnesia, confusion, dysautonomic extrapyramidal reactions (uncontrolled movements of body, including eyes), asthenia, myasthenia gravis during the day, dysarthria, very rarely - paradoxical reactions (aggressive outbursts, fear, suicidal tendencies, muscle cramps, confusion, hallucinations, severe agitation, irritability, anxiety, insomnia). From the side of the SSA: false angina, heart rate, blood pressure reduction. From the side of hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, pain in the throat, excessive fatigue or weakness), anemia, and thrombocytopenia. On the part of the digestive system: dry mouth or salivation, heartburn, abdominal pain, nausea, vomiting, diarrhea or constipation, decreased appetite, liver problems, increased activity of "liver" transaminases and alkaline phosphatase, jaundice. On the part of the genitourinary system: urinary incontinence, urinary retention, renal failure, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Impact on fruit: teratogenicity (especially the I term), CNS depression, respiratory failure and suppression of the sucking reflex in infants whose mothers used the drug. Other: addiction, drug dependency, rarely - inhibition of the respiratory center, blurred vision (diplopia), bulimia, weight loss, tachycardia. With a sharp decrease in dose or cessation of reception - syndrome "cancel" (irritability, headache, anxiety, agitation, excitement, fear, nervousness, sleep disturbances, dysphoria, a spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremors, disorders of perception, including giperakuziya, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare - acute psychosis). overdosage. Symptoms: drowsiness, confusion, paradoxical excitement, reduced reflexes, stupor, decreased response to pain stimuli, deep sleep, dysarthria, ataxia, visual disturbances (nystagmus), tremor, bradycardia, dyspnea or shortness of breath, marked weakness, reduced blood pressure, collapse , inhibition of cardiac and respiratory activity, coma. Treatment: gastric lavage, forced diuresis, receiving activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure, excited by the introduction of barbiturates is not recommended). As a specific antagonist flumazenil use (in a hospital). Hemodialysis is ineffective.

Dosage and administration:
Inside, the smallest effective dose, before bedtime. Adult: 15-30 mg, debilitated patients and in old age - 15 mg, if necessary, taking into account the tolerance dose increases. Treatment duration - 7-10 days.

Cautions:
In the treatment of patients is strictly prohibited the use of ethanol. In renal and / or hepatic insufficiency and prolonged treatment is necessary to monitor the pattern of peripheral blood and liver "enzymes. On the second or third night of consecutive use increased efficiency flurazepama, after stopping for 1 - 2 days, may continue its operation. In the absence of therapeutic effect after 7-10 days of treatment necessary to verify the diagnosis. The risk of drug dependence increases when using large doses, a considerable length of treatment, patients who previously abused drugs or ethanol. Without specific instructions, should not be used for a long time. Do not abrupt discontinuation of treatment because of the risk of the syndrome of "lifting" (headache, myalgia, anxiety, tension, confusion, irritability, and in severe cases - derealization, depersonalization, giperakuziya, photophobia, paresthesia in extremities, hallucinations and seizures). Remove the drug should be gradual. If you have any patients with such unusual reactions, as increased aggressiveness, acute state of excitement, anxiety, suicidal thoughts, hallucinations, increased muscle cramps, difficult to fall asleep, shallow sleep, treatment should be discontinued. During pregnancy, use only in exceptional cases and only emergencies. Toxic effect on the fetus and increase the risk of birth defects when used in the I trimester of pregnancy. Therapeutic dose in the later stages of pregnancy can cause depression of the central nervous system of the newborn. The constant use during pregnancy can cause physical dependence with the development of the syndrome of "cancellation" of the newborn. Children, especially at a younger age, are very sensitive to the depressant drug action of benzodiazepines. Using just before birth or during labor may cause newborn respiratory depression, reduced muscle tone, hypotension, hypothermia and a weak act of sucking (syndrome flaccid child. ") During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Interaction:
Antihistamines, psychoactive drugs, ethanol and etanolsoderzhaschie drugs increase the depressant effect on CNS. Microsomal oxidation inhibitors increase the sedative effect, extend T1 / 2, increase the risk of toxic effects. Inductors of microsomal liver enzymes less efficient. Opioid analgesics enhance the euphoria, leading to the rise of psychological dependence . Antihypertensive drugs - the risk of significant decrease of BP. Against the background of the simultaneous appointment of clozapine may be increased respiratory depression. reduces the effectiveness of levodopa in patients with Parkinson's disease. may increase the toxicity of zidovudine.

Clindamycin

Trade name:
Dalatsin

The international name:
Clindamycin (Clindamycin)

Group Affiliation:
Antibiotic Lincosamides

Description of the active substance (INN):
Clindamycin

Dosage form:
gel for external use, vaginal cream, vaginal suppositories

Mode of action:
Bacteriostatic antibiotic group Lincosamides, has a broad spectrum of activity, binds to the 50S ribosomal subunit of the membrane and inhibits protein synthesis in the microbial cell. In a number of gram-positive cocci may bactericidal action. It is active against Staphylococcus spp. (Including Staphylococcus epidermidis, producing and neprodutsiruyuschih penicillinase), Streptococcus spp. (Except Enterococcus faecalis), Streptococcus pneumoniae, Corynebacterium diphtheriae, Mycoplasma spp., Anaerobic and microaerophilic gram positive cocci (including Peptococcus spp. And Peptostreptococcus spp.), Clostridium perfringens, Clostridium tetani, Bacteroides spp. (Including Bacteroides fragilis and Prevotella melaninogenica), Fusobacterium spp., Propionibacterium spp., Eubakterium and Actinomyces israelii. Most strains of Clostridium perfringens susceptible to clindamycin, but other types of Clostridium spp. (Including Clostridium sporogenes, Clostridium tertium) are resistant to its action in this connection with infections caused by Clostridium spp., Recommended definition antibiotikogrammy. Between clindamycin and lincomycin there is cross-resistance.

Indications:
Vaginal Cream - vaginitis, caused by microorganisms sensitive to drugs. Gel - acne.

Contraindications:
Hypersensitivity, pregnancy trimester I (for vaginal cream).

Adverse effects:
Allergic reactions. Vaginal Cream - irritation at the site of application, cervicitis, vaginitis, the development of superinfection (fungal vaginitis). Gel - irritation (in place of application), contact dermatitis. When resorption is likely to develop systemic side effects, including in rare cases - pseudomembranous enterocolitis.

Dosage and administration:
Vaginal: vaginal cream administered in a single dose - 100 mg clindamycin (1 applicator) for the night, the treatment course - 3-7 days. Outwardly: gel for topical application is applied to the affected area 2-3 times a day.

Cautions:
Vaginal Cream is not recommended for use in conjunction with other intravaginal drugs.

Interaction:
Incompatible with solutions containing a complex of vitamins B, aminoglycosides, ampicillin, calcium gluconate and magnesium sulfate. Be antagonism with erythromycin.

DALACIN C

CLINDAMYCINUM J01F F01
Pfizer Inc.

COMPOSITION AND FORM:

cps. 150 mg, № 16 46.85 grn.

Clindamycin 150 mg

Other ingredients: starch, lactose, talc, magnesium stearate.

Capsule: gelatin, sodium erythrosine, indigotindisulfonat sodium, titanium dioxide.

cps. 300 mg, № 16 60.45 grn.

Clindamycin 300 mg

Other ingredients: starch, lactose, talc, magnesium stearate.

Capsule: gelatin, sodium erythrosine, indigotindisulfonat sodium, titanium dioxide.

№ P.05.01/03065 from 20.03.2006 to 20.03.2010

Pharmacological properties: clindamycin - a semisynthetic antibiotic that is synthesized from lincomycin by replacing 7 - (R)-hydroxyl group of 7 - (S)-chloro.

Depending on the sensitivity of the microorganism and the concentration can act bactericidal or bacteriostatic.

In vitro active against these microorganisms:

- Aerobic Gram-positive cocci, including Staphylococcus aureus, Staphylococcus epidermidis (including strains producing and not producing penicillinase); in vitro saw a rapid development of resistance to the drug in some strains that are resistant to erythromycin; Streptococcus spp. (Except Streptococcus faecalis), Streptococcus pneumoniae;

- Anaerobic Gram-negative bacteria, including Bacteroides spp. (Including B. fragilis, B. melaninogenicus), Fusobacterium spp.;

- Anaerobic Gram-positive asporogenous bacteria, including Propionibacterium, Eubacterium, Actinomyces spp.;

- Anaerobic and microaerophilic Gram-positive cocci, including Peptococcus spp., Peptostreptococcus spp., Microaerophilic streptococci; Clostridium spp. Clostridium are more resistant to clindamycin than most other anaerobes. The majority of clostridia, particularly Clostridium perfringens, are susceptible to clindamycin, but some species (eg C. sporogenes and C. tertium) is often resistant to clindamycin. In connection with this test should be conducted on the sensitivity to antibiotics.

In in vitro studies found that the clindamycin susceptible strains of microorganisms such as Bacteroides melaninogenicus, B. disiens, B. bivius, Peptostreptococcus spp., Gardnerella vaginalis, Mobiluncus mulieris, M. curtisii, Mycoplasma hominis.

Once inside there is a rapid and almost complete (90%) absorption of clindamycin. Simultaneous food intake does not affect the concentration of clindamycin in serum krovi.U adults after oral administration of clindamycin at a dose of 150 mg maximum level of drug in serum (2.5 mg / ml) was achieved after 45 minutes, after 3 h drug concentration is 1.51 ug / ml, and after 6 h - 0,7 mg / ml. Cumulation of the drug in the body or changes its metabolism during prolonged (for 14 days) admission were noted.

The half-life of clindamycin is somewhat increased in patients with severely impaired renal function. Hemodialysis and peritoneal dialysis for removing clindamycin from the blood are not effective. The concentration of clindamycin in the serum increased linearly with the increase of the dose. Serum concentration of drug within 6 h after administration of the usual dose exceeds the minimum inhibitory concentration on most of the above mikroorganizmov.Klindamitsin broadly distributed in tissues and body fluids (including a bone). The average biological half-life of 2.4 h. Approximately 10% of the active drug is excreted in urine, 3,6% - with the feces, the remainder of the drug is released in the form of inactive metabolites. Acceptance of clindamycin at a dose of 2.0 g over 14 days was well tolerated; healthy volunteers, albeit at higher doses was observed an increase in the frequency of side effects from the digestive tract. In the CSF, even against the background of inflammatory process significant concentrations of clindamycin were not met. Ingestion of clindamycin hydrochloride in elderly patients showed an increase in the average half-life of up to 4 h (range 3,4-5,1 h), compared with a group of younger patients - 3.2 hours (range 2.1 - 4,2 h). However, the extent of absorption in different age groups did not differ significantly, so no need to adjust the dose of the drug in elderly patients with intact function of the liver and kidneys.

INDICATIONS: infectious-inflammatory diseases caused by microorganisms sensitive to clindamycin:

- Infection of lower respiratory tract, including bronchitis, pneumonia, lung abscess, empyema;

- Infections of skin and soft tissues, including acne, furunculosis, abscess, impetigo, abscesses, infected wounds, specific infectious processes of the skin and soft tissues (erysipelas, and paronychia / felon);

- Infections of bones and joints, including osteomyelitis and suppurative arthritis;

- Gynecological infections, including endometritis, abscess, coleitis, salpingoophoritis, pelviotsellyulit, pelvioperitonit;

- Infectious processes in the abdominal cavity, including peritonitis, abscesses of the abdominal cavity (in combination with antibiotics, acting on Gram-negative aerobes);

- Septicemia and endocarditis;

- Infection of oral cavity, including periodontal abscess and periodontitis;

- Toxoplasma encephalitis in AIDS patients (proof of efficacy of clindamycin in combination with pyrimethamine in patients with intolerance to standard therapy);

- Pneumocystis pneumonia in AIDS patients (patients who can not tolerate or are resistant to standard therapy, clindamycin may be used in combination with primaquine);

- Malaria, including cases caused by MDR Plasmodium falciparum (alone or in combination with quinine or chloroquine);

- Prevention of endocarditis in patients with hypersensitivity to penicillins.

APPLICATION: dose depends on the severity of the disease, the patient's condition and the sensitivity of a pathogen to the antibiotic.

Adults appoint a dose of 600-1800 mg / day, divided into 2, 3 or 4 equal doses. To avoid irritation of the mucous membrane of the esophagus capsules should be taken with a full glass of water.

The dose of clindamycin hydrochloride for children over 6 years of age is 8-25 mg / kg / day in 3-4 reception within 7-10 days.

Corrections of dose in the elderly, as well as in patients with hepatic or renal insufficiency is not required.

For infections caused by β-hemolytic streptococcus, treatment should continue for at least 10 days. In acute streptococcal tonsillitis / pharyngitis dose of clindamycin hydrochloride for oral administration of 300 mg 2 times a day for 10 days.

In the treatment of pelvic inflammatory disease after parenteral reference drug for 6 days should continue receiving clindamycin hydrochloride oral dose of 450-600 mg every 6 h until the completion of 10-14 day cycle of therapy.

With cervical infection caused by Chlamydia trachomatis, is prescribed in doses of 450-600 mg by mouth 4 times a day for 10-14 days.

In Toxoplasma encephalitis in AIDS patients clindamycin hydrochloride prescribe oral dose of 600-1200 mg every 6 h for 2 weeks, then 300-600 mg orally every 6 hours Usually therapy is 8-10 weeks. The dose of pyrimethamine 25-75 mg orally every day for 8-10 weeks. In the application of pyrimethamine in higher doses should be administered folinievuyu acid in a dose of 10-20 mg / day.

When pneumocystis pneumonia in AIDS patients clindamycin hydrochloride administered in a dose of 300-450 mg orally every 6 hours for 21 days and primaquine at a dose of 15-30 mg orally 1 time a day for 21 days.

When malaria in adults prescribed a dose of 10-20 mg / kg per day, the children - 10 mg / kg / day in equal doses every 12 hours for 7 days as monotherapy or in combination with quinine (12 mg / kg every 12 h) or hlorohininom (15-25 mg every 24 h) for 3-5 days.

In order to prevent endocarditis in patients with hypersensitivity to penicillin adults prescribe 600 mg 1 hour prior to surgical or medical diagnostic procedures (eg tonsillectomy, adenoidektomii, bronchoscopy, rigid bronchoscopy, dilatation of the stricture of the esophagus, retrograde cholangiopancreatography, cystoscopy, etc.) ; children - 20 mg / kg for 1 h before the procedure.

CONTRAINDICATIONS: Hypersensitivity to clindamycin, lincomycin, or other components of the drug, myasthenia gravis, the age of 6 years.

SIDE EFFECTS: transient neutropenia / leukopenia, eosinophilia, agranulocytosis, thrombocytopenia (a distinct causal connection with the use Dalatsina C is not installed); anaphylactoid reaction, dysgeusia, abdominal pain, nausea, vomiting, diarrhea, esophagitis, esophageal ulcers, jaundice, changes indicators of hepatic functional tests (including hyperbilirubinemia), maculopapular rash, urticaria, small or moderate generalized rash, erythema polymorphous syndrome, Stevens - Johnson, itching, vaginitis, exfoliative, and vesicle-bullous dermatitis, toxic epidermal necrolysis.

Cautions: The treatment of clindamycin, as well as other antibiotics, may be complicated by the development of pseudomembranous colitis. It is therefore important to diagnose this pathology in patients with diarrhea during treatment with antibacterial drugs and repeal the drug.

Clindamycin should not be appointed for the treatment of meningitis because the drug enters the CSF poorly.

If the treatment is done for a long time, in this case it is necessary to control the function of liver and kidneys. Because clindamycin therapy may occur activation microflora, insensitive to the drug, especially yeast flora.

Clindamycin crosses the placenta. Prolonged use of drug concentration in the amniotic fluid is 30% of its concentration in maternal blood. Dalatsin C can be used for treatment of pregnant women only when absolutely necessary. Reported the detection of clindamycin in human breast milk in concentrations of 0,7-3,8 mg / ml. Dalatsin C can be used for women who are breastfeeding, unless absolutely necessary.

INTERACTION: in vitro found that clindamycin and erythromycin are the antagonists in this connection is not recommended to co-administration of these drugs. Between clindamycin and lincomycin there is cross-resistance.

The drug is incompatible with ampicillin, barbiturates, aminophylline, calcium gluconate, magnesium sulfate. The simultaneous use of antidiarrheal drugs increases the risk of pseudomembranous colitis.

Dalatsin C has the ability to block neuromuscular transmission and may enhance the action of other neuromuscular blockers, and the drug should be used with caution in patients who are prescribed muscle relaxants.

OVERDOSE: Overdose of the drug has no specific clinical manifestations. No specific antidote. Hemodialysis or peritoneal dialysis are ineffective.

STORAGE: at room temperature (15-25 ° C).