tomoxifen

Combined saline solution for rehydration and detoxification. It provides hemodynamic effects, reducing hypovolemia, preventing blood clots tomoxifen and the development of metabolic acidosis, improves capillary blood circulation, enhances diuresis and has a detoxication effect.

Indications
Rehydration, intoxication on the background of dehydration (including cholera, acute dysentery, food poisoning).

Contraindications:
Hypersensitivity, hyperkalemia, renal and heart failure, alkalosis.

Dosing and Administration
Intravenous (bolus and infusion), under tomoxifen the control of laboratory parameters. Within 1 hour the solution was injected in an amount corresponding to 7 – 10% of the body weight of the patient; then replaced bolus drip for 24 – 48 hours at 40 – 120 drops / min. Before the introduction of the solution warmed to 36 – 38 ° C. The solution was administered in an amount necessary to restore the fluid volume lost with feces, vomit, urine and sweat. Balance imposed and the lost fluid is determined every 6 hours.

Side effects:
swelling, tachycardia, hyperkalemia. Rarely – chills.

Cautions
therapy is performed under the control of the hematocrit and blood electrolyte concentration.
With the development of hyperkalemia solution can be replaced with a solution “Disol” to normalize the electrolyte balance.

Product form
Solution for infusion of 200 or 400 ml tomoxifen in glass bottles for blood, infusion and transfusion products with a capacity of 250 or 450 ml, respectively, sealed with rubber stoppers and crimped aluminum caps.
For one bottle with instructions for use and gasket made of corrugated cardboard is placed in a carton pack.
20 bottles of 250 ml or 15 bottles of 450 ml capacity with 5 – 10 copies of the instructions for use in a cardboard box (for hospitals).

tamoxifin

You can not assign during transport drivers and others persons, professions that require high concentration and speed of psychomotor reactions. During treatment it is necessary to monitor blood pressure, pulse, regularly monitor liver function, kidney and blood. Patients should not be exposed to tamoxifin radiation, because the drug can cause photosensitivity. During treatment should avoid the use of ethanol.

Interaction : With simultaneous use of chlorpromazine with other drugs, have a depressing effect on the central nervous system (funds for general anesthesia, opioids, ethanol (alcohol) and containing its drugs, barbiturates, tranquilizers, and others.) May increase  depression and respiratory depression;
undesirably prolonged combination with analgesics and antipyretics – may develop hyperthermia;
tricyclic antidepressants, maprotiline, or tamoxifin inhibitors – increase the risk of neuroleptic malignant syndrome;
with anticonvulsants – may decrease the seizure threshold,
with preparations for the treatment of hyperthyroidism – increased risk of agranulocytosis;
other drugs cause extrapyramidal reactions – may increase the frequency and severity of extrapyramidal disorders; with antihypertensive drugs – possible orthostatic hypotension
with ephedrine – may weaken the vasoconstrictor effect of ephedrine. When treating chlorpromazine avoid administration of epinephrine (adrenaline), since distortion may effect epinephrine, which can lead to a drop in blood pressure. Antiparkinsonian effect of levodopa tamoxifin is reduced due to the blocking of dopamine receptors. Aminazin can suppress the effect of amphetamines, clonidine, guanethidine. Aminazin enhances anticholinergic effects of other drugs, and the antipsychotic effect of neuroleptics may be reduced. With simultaneous use of chlorpromazine with a related chemical structure prochlorperazine may come a long unconsciousness. Antacids, antiparkinsonian drugs, and lithium salts may reduce the absorption of chlorpromazine, besides combination with lithium therapy increases the risk of extrapyramidal complications.
Chlorpromazine may mask some of the manifestations tamoxifin of ototoxicity (tinnitus, vertigo) of drugs that have ototoxic effects (eg. Antibiotics with ototoxic effect) . Other hepatotoxic drugs increase the risk of hepatotoxicity.

 

tamoxifen

Drops chlorpromazine prescribed inside , without chewing, drinking plenty of water.
The initial daily dose for oral tamoxifen administration of 25-100 mg / day, 1-4 times a day, then, subject to tolerability, the dose is gradually increased to 25-50 mg every 3-4 days, until the desired therapeutic effect. In the case of the low efficiency of moderate doses of chlorpromazine, a dose increase to 700-1000 mg / day, in some cases, extremely resistant without somatic contraindications dose can be increased up to 1200-1500 mg / day. In the treatment with high doses, the daily dose is divided into 4 parts (the latter – before going to bed). Duration of treatment with high doses should not exceed 1-1.5 months, in the absence of the effect it is advisable to go to the treatment of other drugs.
Higher doses of chlorpromazine for adults inside: single 0.3 g daily 1.5 g chlorpromazine Children appoint depending on age: more than 3 years and older into 550 ug / kg (0.55 mg / kg) or 15 mg per 1 m of the body surface, if necessary every 6-8 hours children 3 years – 5 years (body weight 23 kg. ) should not be given more than 40 mg per day; children 5-12 years of age (body weight 23 to 46 kg) should not be administered more than 75 mg per day.
For use in pediatric dosage forms appropriate to use for children.
Impaired and elderly patients, depending on the age, prescribed to 0.3 g / day.

Side effects :
At the beginning of treatment tamoxifen may experience drowsiness, dizziness, dry mouth, anorexia, constipation, paresis of accommodation, moderately severe orthostatic hypotension, tachycardia, insomnia, urinary retention, reduced potency, frigidity, allergic reactions of the skin and mucous membranes ( photosensitivity), angioneurotic edema of the face and extremities); at least – a sharp decrease in blood pressure.With prolonged use of high doses (0.5-1.5 g / day) – extrapyramidal disorders (dyskinesias – paroxysmally arising convulsions neck muscles, tongue, floor of the mouth, akinetorigidnye effects, akathisia, hyperkinesia, tremor and autonomic disorders), psychic phenomena indifference, a belated reaction to external stimuli, neuroleptic depression and others. mental changes, cholestatic jaundice, cardiac arrhythmias, lymph and leukopenia, anemia, agranulocytosis, hypercoagulation, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, nausea, vomiting, diarrhea, oliguria, skin pigmentation, blurred lens and cornea; in rare cases – seizures (as correctors used antiparkinsonian agents – tropatsin, trihexyphenidyl, etc .; dyskinesia tamoxifen cropped s / c administration of 2 ml of a 20% solution of caffeine sodium benzoate and 1 ml of 0.1% solution of atropine), neuroleptic malignant syndrome.

Overdose (intoxication) drug
Symptoms: areflexia and hyperreflexia, blurred vision, cardiotoxic effects (arrhythmia, heart failure, decreased blood pressure, shock, tachycardia, changes , ventricular fibrillation, cardiac arrest), neurotoxic effects, including agitation, confusion, convulsions, disorientation, lethargy, stupor or coma; dilated pupils, dry mouth, hyperpyrexia or hypothermia, muscle rigidity, vomiting, pulmonary edema and respiratory depression. Treatment: gastric lavage, the appointment of activated charcoal (to avoid the induction of vomiting as impaired consciousness, and dystonic reactions from the muscles tamoxifen of the neck and the head, caused by an overdose may lead to aspiration of vomit). Symptomatic treatment: arrhythmia – in / phenytoin 9-11 mg / kg, in heart failure – cardiac glycosides, with marked decrease in blood pressure – in / in a liquid or vasopressor agents such as norepinephrine, phenylephrine (avoid the use of alpha and beta -adrenomimetikov such as epinephrine as possible paradoxical decrease in blood pressure by blocking the alpha-adrenoceptor chlorpromazine), in convulsions – diazepam (barbiturates avoided due to possible subsequent depression  and respiratory depression), parkinsonism – difeniltropin, diphenhydramine. CCC Control functions for at least 5 days, the central nervous system, respiration, body temperature measurement, consulting psychiatrist. Dialysis is ineffective.

side effects of tamoxifen

Well absorbed and rapidly after the / m and by ingestion. Bioavailability after oral administration – 50%. Cmax in plasma achieved in 1-2 hours – after the / m and 2-4 hours after ingestion. Relationship to plasma proteins – 90-99%. Nonuniformly accumulated in various organs. Easily penetrate the  while its concentration in the brain than in plasma concentration. There is no direct correlation between plasma concentration and therapeutic effect. Has the effect of “first pass” through the liver where the drug is extensively metabolized by oxidation (30%), hydroxylation (30%) and dezametilirovaniya (20%). Possess pharmacological activity oxidized hydroxylated metabolites that are inactivated by binding with glucuronic acid, either by further oxidation to form sulfoxides inactive. Excreted by the kidneys and the bile. Side effects of tamoxifenper day output of about 20% of the dose, 1-6% of the dose excreted by the kidneys unchanged. Traces of metabolites found in the urine after 12 months or more after stopping treatment. Due to the high protein binding is not substantially subjected to dialysis.

Indications : In psychiatry, – psychomotor agitation (including patients with schizophrenia); acute delirium, manic and hypomanic excitement in manic-depressive psychosis, chronic psychosis; mental diseases of various origins, accompanied by fear, anxiety, agitation, insomnia; psychopathy (including in patients with epilepsy and organic diseases of the central nervous system), alcoholic psychosis. Severe nausea and vomiting, persistent hiccups. To enhance the analgesic action for persistent pain. Diseases accompanied by increased muscle tone: after cerebrovascular, tetanus , and others.

Contraindications :

 

  • increased individual sensitivity;
  •  depression and coma function of any etiology;
  • brain injury;
  • liver disease, kidney and blood-forming organs in violation of the functions;
  • progressive system of the brain and spinal cord diseases;
  • gastric ulcer and 12 duodenal ulcer during the exacerbation;
  • heart disease in the stage of decompensation (heart disease, myocardial dystrophy, rheumatic heart disease, etc.), severe hypotension, diseases accompanied by the risk of thromboembolic complications;
  • bronchiectasis in the stage of decompensation;
  • angle-closure glaucoma side effects of tamoxifen (risk of increased intraocular pressure);
  • prostatic hyperplasia;
  • myxedema;
  • pregnancy, breast-feeding;
  • children up to 3 years.With caution :
    Parkinson’s disease, active side effects of tamoxifen alcoholism (the risk of hepatotoxic effects), breast cancer, epilepsy, chronic diseases accompanied by respiratory failure (especially in children), Reye’s syndrome, cachexia, old age, vomiting (antiemetic effect of phenothiazines may mask vomiting, associated with overdose al. drugs).

tamoxifen side effects

The action of proteolytic enzyme preparation derived from the pancreas of cattle. Hydrolysis of proteins and peptones to form relatively low molecular weight peptides, cleaves bonds formed by the remains of aromatic amino acids (tyrosine, tryptophan, phenylalanine, methionine).
In clinical practice, the use of chymotrypsin is based on the specific features of break down necrotic tissue and fibrinous formation dilute viscous secrets and exudates, and when administered intramuscularly to provide anti-inflammatory effect.

Indications for use.
Suppurative disease of the tamoxifen side effects respiratory system (tracheitis, bronchitis, bronchiectasis, pneumonia, lung abscess, atelectasis, pleural effusion, asthma).
In the treatment of burns, pressure ulcers, festering wounds, thrombophlebitis.
In ophthalmology – with fresh extensive thrombosis of the central vein retina, acute obstruction of the central retinal artery, vitreous opacities traumatic and inflammatory origin, cataract extraction.
In otolaryngology – purulent sinusitis, subacute laryngo-tracheitis, after tracheostomy to facilitate removal of the thick viscous exudate, acute, subacute, suppurative, chronic otitis media and evstahiitah viscous exudate.

Contraindications
: Hypersensitivity to chymotrypsin, cancer, pulmonary tuberculosis (open form), chronic heart failure II -. III degree dystrophy and cirrhosis, viral hepatitis, pancreatitis, hemorrhagic diathesis, emphysema, respiratory failure
can not enter into the bleeding cavity, apply ulcerated on the surface of malignant tumors in order to avoid the spread of malignancy.

Be wary.
Empyema of tubercular etiology (absorption of exudate may in some cases contribute to the development of bronchopleural fistula).

Pregnancy and lactation
Data on the use of the drug during pregnancy and lactation is not.

Dosing and Administration.
For intramuscular dissolve immediately before use 0.005 g in 1 to 2 mL of sterile 0.9% sodium chloride solution or 0.5-2% procaine solution. Treatments -. 6-15 injections
In respiratory diseases, drug use intramuscularly in doses of 5-10 mg per day for 10-12 days, can be combined with aerosol chymotrypsin in 5% aqueous solution in an amount 3-4ml. After 7-10 days of treatment may be repeated.
In the treatment of burns and bedsores chymotrypsin at a dose of 20 mg was dissolved in 20 ml of 0.25% solution of procaine and a few thin needle pricks is injected under the scab. In purulent wound surfaces applied 8 hours, sterile wipes, moistened with a solution of 0.025-0.05 g chymotrypsin in 10-50 ml of 0.25% solution of procaine. For the treatment of purulent wounds intramuscular injection combined with local treatment of the wound swab dipped 5% aqueous solution of chymotrypsin.
When thrombophlebitis drug is given intramuscularly at 5-10 mg daily for 7-10 days.
When extraction chymotrypsin cataract in a dilution of 1: 5000 is introduced in posterior chamber of the eye, followed by washing the anterior chamber of 0.9% sodium chloride solution after 4 minutes after administration.
In the treatment of central retinal vein thrombosis, acute obstruction of central artery of retina chymotrypsin subconjunctival administered 0.2 ml of a 5% solution prepared by 1 % solution of procaine, 1-2 times a week.
When the drug is administered in sinusitis corresponding cavity in an amount of 5-10 mg in 3-5 ml of 0.9% sodium chloride and after puncture cavity tamoxifen side effects lavage.
When otitis buried in the ear to 0, 5-1 ml of 0.1% solution of chymotrypsin of 0.9% sodium chloride solution. At the micro-operations on the ear to soften fibrinous formations in the middle ear during surgery injected into the cavity of 0.1% chymotrypsin solution. Simultaneously chymotrypsin should be administered intramuscularly 2.5-5 mg 1-2 times a day. The drug is diluted in 1-2 mL of 0.25-0.5% solution of novocaine or 0.9% sodium chloride solution.

Side effect
May cause allergic reactions, fever up to subfebrialnoy, tachycardia
After inhalation: occasionally observed irritation of the mucous membranes of the upper airways, hoarseness.
When tamoxifen side effects subconjunctival administration may result in irritation and swelling of the conjunctiva; in such cases it is advisable to reduce the concentration of the solution.
After intramuscular administration may be soreness and redness at the injection site.