Pulmonary tuberculosis and other tuberculosis
Dosage regimen
Usually adults are intramuscularly or intravenously injected as isoniazid in a daily dose of 200 to 500 mg (4 to 10 mg / kg) <4 to 10 mL>. For intrathecal, intrathoracic injection or local dispensation, use 50 to 200 mg <1 to 4 mL> once.
Change according to age and symptoms as appropriate.
It is desirable to use it in combination with other anti-tuberculosis drugs.
Usage notes
Careful Administration
Liver disorder or its past history or a patient suspected of it [Liver disorder may deteriorate or recur. ]
Patients with kidney disorder or suspected dysfunction [Increase blood levels of this drug, which is likely to cause side effects such as peripheral neuritis. ]
Patients with a history of mental disorders [Psychiatric disorders may recur. ]
Patients with alcoholism [liver disorder, psychiatric disorder may occur]. ]
Patients with convulsive disorders such as epilepsy or those with a history of these [It is possible to cause convulsions, so if it is inevitable to administer observe thoroughly. ]
Patient with drug hypersensitivity
Patients with blood disorders, bleeding tendencies [These symptoms may be exacerbated. ]
Important basic attention
Severe hepatic disorder may occur by combination with other anti-tuberculosis drugs. Therefore, when using in combination, conduct a liver function test at regular intervals (see "Serious side effects").
Side effect
Outline of side effect development
(Not subject to reexamination)
Serious side effects and side effect terms
Serious side effects
(Frequency unknown Note 1))
The following serious side effects may appear, so observe thoroughly, if abnormalities are observed discontinue administration and take appropriate measures.
Serious liver disorder such as fulminant hepatitis
To perform liver function test on a regular basis.
Toxic epidermal necrolysis (TEN), skin mucosa ocular syndrome (Stevens-Johnson syndrome), erythroderma (exfoliative dermatitis)
Drug hypersensitivity syndrome [1]
(Initial symptoms: rash, fever)
(Secondary findings: liver dysfunction, lymph node swelling, leukocytosis, eosinophilia, emergence of atypical lymphocytes, etc.)
Be aware that frequent revitalization of viruses such as Human Herpesvirus 6 (HHV-6) is frequent and symptoms such as rash, fever, liver dysfunction may recur or prolong even after administration is discontinued.
SLE-like symptoms
(Symptoms: fever, erythema, muscle pain, arthralgia, lymph node swelling, chest pain etc.)
(Treatment method: adrenocortical hormone drug administration etc.)
Interstitial pneumonia
(Symptoms: fever, cough, dyspnea, chest x-ray abnormality, eosinophilia etc.)
(Treatment method: adrenocortical hormone drug administration etc.)
Renal failure, interstitial nephritis, nephrotic syndrome
(Symptoms: fever, rash, oliguria, edema, proteinuria, renal function test value abnormality etc.)
Agranulocytosis, thrombocytopenia
convulsions
Optic neuritis
(Symptoms: visual acuity reduction, central scotoma etc.)
(Treatment method: administration of vitamin B 6 etc.)
Peripheral neuritis
(Symptom: abnormal sensation of limbs, numbness, sensory disorder, decreased tendon reflex, muscle weakness, muscle atrophy etc.)
(Treatment method: administration of vitamin B 6 etc.)
Administration to the elderly
In general elderly people have decreased physiological function, so be careful not to lose weight etc.
Administration to pregnant women, maternity women, nursing women, etc.
It is advisable not to administer to pregnant women or lactating women who may be pregnant. [An animal experiment (mouse) reports the fetal growth hindrance effect. There is also epidemiological findings that patients with aminosalicylate formulation are administered concomitantly, and the incidence of malformed children is high. ]
To lactating women should avoid breast feeding during this drug administration. [It may migrate into human breast milk. ]
Overdosage
The following reports are reported by oral administration of isoniazid.
Symptom
Convulsions, coma, metabolic acidosis, hyperglycemia may occur.
treatment
Diazepam is administered for suppression of convulsions and sodium bicarbonate is injected intravenously for metabolic acidosis.
Secure the respiratory tract and ensure adequate respiration.
Intravenously inject the same amount of pyridoxine as isoniazid dose.
In severe cases, it is desirable to perform blood perfusion or hemodialysis.
Application note
During intramuscular injection
When intramuscular injections, please pay attention to the following points in order to avoid influences on tissues, nerves, etc.
For the injection site, careful administration should be avoided avoiding the nerve running site.
In case of repetitive injections, avoid the same parts by injecting left and right alternately. Beware of low birth weight infants, newborns, infants, young children, and children.
When injecting a needle, if you complain of severe pain or seeing backflow of blood, immediately remove the needle, change the site and inject it.
At opening
To avoid contamination of ampule at the time of foreign matter, wipe with ethanol disinfecting cotton etc and cut it.
Other notes
The occurrence of lung tumor has been reported in an experiment with mice [example: 0.01 to 0.25% contamination in feed (about 15 to 375 mg / kg body weight orally for 7 months)]. However, tumor-inducing effects have not been reported in experiments with rats and hamsters. Also, epidemiological findings reporting that no association with tumor development was observed in humans has been reported.
Pharmacokinetics
Protein binding [2]
Isoniazid binds to serum proteins (mainly albumin), and the molar ratio of isoniazid bound per 1 mol of human serum albumin was 0.08.
metabolism
After dosing, isoniazid was mostly acetylated in the liver, became 1-acetyl-2-isonicotinylhydrazine, was further metabolized, and became 1,2-diacetylhydrazine and acetylhydrazine and was excreted in the urine [3] 4].
There is genetic diversity (rapid or slow acetylator) in this metabolic rate of N-acetylation, and racial differences are seen (Japanese and slow acetylator is less than 10%).
Medicinal pharmacology
Antimicrobial power [5]
The minimum inhibitory concentration (MIC) against M. tuberculosis H37 Rv strain is 0.1 μg / mL (measured in 10% serum Kirchner medium).
Also, a remarkable therapeutic effect is recognized for mouse experimental tuberculosis (H37Rv strain).
Physicochemical knowledge on active ingredients
common name: Isoniazid
Common name (European name): Isoniazid
Abbreviated name: INH
Chemical name: Pyridine-4-carbohydrazide
Molecular formula: C 6 H 7 N 3 O
Molecular weight: 137.14
Melting point: 170 - 173 ° C
Property: It is colorless crystal or white crystalline powder, it has no odor. It is easily soluble in water or acetic acid (100), slightly soluble in ethanol (95), hardly soluble in acetic anhydride, and very insoluble in diethyl ether.
Handling Precautions
Since this product uses "one-point cut ampule", fold in the opposite direction with the mark of the ampoule branch up.
Packaging
Iscotin Note 100 mg (Japanese Pharmacopoeia Isoniazid injection)
(2 mL) 20 ampoules
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