Stamp: [THE MINISTRY OF HEALTH OF RUSSIA
ЛП001899-091112
APPROVED]
THE MINISTRY OF HEALTH
OF THE RUSSIAN FEDERATION
BASIC PRESCRIPTION INFORMATION
for the medical drug
Perchlozone®
Registration No.:
Trade Name: Perchlozone
International Nonproprietary Name: Thioureidoiminomethylpyridinium perchlorate
Dosage Form:
film-coated tablets
Composition:
Active Ingredient:
Thioureidoiminomethylpyridinium perchlorate (Perchlozone) 200 mg, 400 mg
Excipients:
Core: silicon dioxide colloidal 5.0 mg/10.0 mg, crospovidone 17.5 mg/35.0 mg, magnesium
stearate 2.5 mg/5.0 mg, povidone 5.0 mg/10.0 mg, microcrystalline cellulose 60.0 mg/120.0 mg.
Film coat: hypromellose E5 0.35 mg/0.70 mg, hypromellose E15 6,0 mg/12.0 mg, yellow iron
oxide 0.40 mg/0.80 mg, macrogol 6000 1.25 mg/2.5 mg, talcum 1.0 mg/2.0 mg, propylene glycol
0.50 mg/1.0 mg, titanium dioxide 0.50 mg/1.0 mg.
Description
Tablets 200 mg: round biconvex film-coated tablets of yellow to dark yellow colour engraved
with ‘PHZ’ on one side.
At the cross-section the tablet is of pale yellow to yellow colour with a greenish tint.
Tablets 400 mg: oval biconvex film-coated tablets of yellow to dark yellow colour engraved with
‘PHZ’ on one side.
At the cross-section, the tablet is of pale yellow to yellow colour with a greenish tint.
Therapeutic category: antituberculosis agent.
ATC code: J04AK
Pharmacological Properties
Pharmacodynamics
An antituberculosis agent. The mechanism of action hasn’t been established.
The drug is active against Mycobacterium tuberculosis and Mycobacterium bovis. Exerts evident
inhibiting action on the viability of the Mycobacteria tuberculosis including those which are
resistant to other antituberculosis drugs.
Perchlozone is a low-toxic drug which doesn’t induce significant structural or functional
disturbances in the vital organs and systems, neither does it induce irritant effect on the mucous
membranes of the gastrointestinal tract.
The mechanism of action hasn’t been established to the full extent, the study is ongoing.
Pharmacokinetics
Once orally administered Perchlozone is quickly absorbed in the gastrointestinal tract. The time
to peak concentration in the blood (TCmax) is 1.5-3 hours. After oral administration as a single
dose of 400 mg, 800 mg, 1200 mg or 1600 mg the peak concentration in the blood (Сmax) comes
to 2.61±0.34 µg/ml, 5.07±0.69 µg/ml, 5.42±0.65 µg/ml, and 8.17±1.91 µg/ml respectively. The
half-life is 12-27 hours. The time to steady state concentration (Css) of the active ingredient in the
blood with long-term administration comes to 14 days. With the drug being administered as a
course (once a day), the active ingredient concentration in the blood when measured 15 minutes
before a regular dose intake is 23.4 µg per 1 ml of the blood plasma.
The metabolic pathways of the active ingredient haven’t been established, the study is ongoing.
Indications
Pulmonary tuberculosis including the cases with multidrug resistance of the Mycobacteria
tuberculosis (as a part of combination therapy).
Contraindications
Hypersensitivity to the active ingredient or any other components of the drug, impaired liver
and/or kidney function (application of the drug in such patients hasn’t been studied), pregnancy,
breast feeding, children (under 18 years old).
Warnings
Elderly patients.
Pregnancy and Breastfeeding
The drug is contra-indicated to be used in pregnant or breastfeeding patients.
Dosage and Administration
The drug is to be taken orally, once a day after meal. The drug is administered to adults at 9.512.5 mg/kg/day: 400-600 mg/day with the body weight less than 50 kg; 800-1000 mg/day with
the body weight of 50-80 kg; not more than 1200 mg/day with the body weight more that 80 kg.
The duration of the therapy is up to 3 months.
Adverse Effects
Nervous system: vertigo, headache, weakness, sleepiness, loss of consciousness, neuropsychic
reactions (aggression, depression).
Cardiovascular system: tachycardia, palpitation, blood pressure decrease.
Digestive system: pain in the epigastrium, liver transaminase activity increase, nausea, vomiting.
Allergic reactions: itch, rash, dermahemia, toxic allergic reactions, angioneurotic edema.
Other: bronchospasm, fever, eosinophilia, hot flash.
Overdosage
There are no available data on acute overdosage associated with Perchlozone intake in human.
Treatment: specific antidote is unknown. In case of an overdosage, general supportive therapy
with control of the basic physiological parameters is needed.
It is recommended to perform gastric lavage and to administer activated carbon.
Drug Interactions
Interaction with other drugs hasn’t been studied to the full extent.
With simultaneous administration of Perchlozone with other antituberculosis drugs (isoniazid,
amikacin, rifabutin, rifampicin) increase in the activity against Mycobacteria tuberculosis is
observed. At that, it is important to consider possible potentiation of the adverse effects.
Special Instructions
In case of occurrence of allergic reactions it is recommended to withdraw the drug. Do not use
metamizole sodium (analgin) for the purpose of relieving fever. In case of occurrence of other
abovementioned adverse reactions, it is recommended to consider the possibility of reducing the
dose to 400 mg/day or withdrawal of the drug.
Effects on ability to drive and use machines
No specialized study of the Perchlozone effects on the ability to drive and use machines was
performed. Such adverse events as vertigo, weakness, sleepiness (see the section Adverse
Effects) can impair reactivity and the ability to concentrate attention. During the Perchlozone
therapy, it is recommended to avoid driving and doing potentially dangerous activities requiring
high level of attention and high rate of psychomotor reactions.
Presentation:
200 mg, 400 mg film-coated tablets.
Primary package of the drug product
10 tablets are packed in each blister made of PVC film and printed laminated aluminium foil.
50 or 100 tablets are placed in each polymer jar with a tamper-evident pull-off cap. The free
space is filled with medical absorbent cotton. Stickers made of tag/writing paper or of polymeric
materials are attached to the jars.
Secondary package of the drug product
5 or 10 blisters along with a package insert are placed in a pack made of carton for consumer
containers of ‘chrome’ or ‘chrome-ersatz’ categories, or other of similar quality. The packs are
placed into a multipack, a box made of corrugated cardboard.
Shelf-life
2 years. Do not use after the expiry date which is stated on the package.
Storage
Store in a dry place protected from light, do not store above 25ºС.
Keep away from children.
Dispensing Terms
Rx.
Manufacturer
JSC Pharmasyntez, Russia.
Registered address: office 3, building 23, Krasnogvardeyskaya street, Irkutsk, 664007, Russia.
Facility address: 1 floor, building 184, R. Luxemburg street, Irkutsk, 664040, Russia.
Consumer complaints to be addressed to:
JSC Pharmasyntez, building 184, R. Luxemburg street, Irkutsk, 664040, Russia,
tel.: (3952) 55-03-55, fax: (3952) 55-03-25.
General director
JSC Pharmasyntez
Stamp: [JOINT STOCK COMPANY PSRN 1023801426538 * IRKUTSK* PHARMASYNTEZ
FOR REGISTRATION DOCUMENTS]
O.V. Turchaninova
/signed/
2012
Stamp: [THE MINISTRY OF HEALTH OF RUSSIA
ЛП001899-091112
APPROVED]
Stamp: [bound and numbered /5/ page(s)
General director
Pharmasyntez JSC
O.V.Turchaninova
/signed/
/30.10.2012/]
Stamp: [JOINT STOCK COMPANY PSRN 1023801426538 * IRKUTSK* PHARMASYNTEZ
FOR REGISTRATION DOCUMENTS]