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MOXAID SODIUM 500MG POWDER FOR SOLUTION FOR INJECTION

Active substance(s): ACETAZOLAMIDE

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Date of Approval:

PROOF

4

To be implemented by:

12/09/2014
Product Description:

Originated by

Date:

MoxaidTM Sodium 500mg Powder for Soln. for Inj.

SMT

08/08/2013 No

Tech Approved

Component:

Revised by

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Leaflet (Health Professional’s)

PAT

XXXXXX/HPL/1

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CRF No.:

BAG

XXXXXXHPL Moxaid PowInj v1_4

QA.CRF.107.2013

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UK

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7.5pt Swiss 721BT

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4.9 Overdose
No specific antidote. Supportive measures with correction of electrolyte and
fluid balance. Force fluids.

5. PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic Properties
Pharmacotherapeutic group: Carbonic anhydrase inhibitors. ATC Code: S01EC01.
Acetazolamide is an inhibitor of carbonic anhydrase. By inhibiting the reaction
catalysed by this enzyme in the renal tubules, acetazolamide increases the
excretion of bicarbonate and of cations, chiefly sodium and potassium, and so
promotes alkaline diuresis.
Continuous administration of acetazolamide is associated with metabolic
acidosis and resultant loss of diuretic activity. Therefore the effectiveness of
MOXAID Injection in diuresis diminishes with continuous use.
By inhibiting carbonic anhydrase in the eye acetazolamide decreases intraocular pressure and is therefore useful in the treatment of glaucoma.

5.2 Pharmacokinetic Properties
Acetazolamide has been estimated to have a plasma half-life of about 4 hours.
It is tightly bound to carbonic anhydrase and accumulates in tissues containing
this enzyme, particularly red blood cells and the renal cortex. It is also bound to
plasma proteins. It is excreted unchanged in the urine, renal clearance being
enhanced in the alkaline urine.

5.3 Preclinical Safety Data

1. NAME OF THE MEDICINAL PRODUCT
MOXAID Sodium 500mg Powder for Solution for Injection
Acetazolamide 500mg Powder for solution for Injection.

2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Each vial contains Acetazolamide 500mg
For full list of excipients see section 6.1.

3. PHARMACEUTICAL FORM
White to off-white powder for solution for injection.

4. CLINICAL PARTICULARS
4.1 Therapeutic Indications
Acetazolamide is an enzyme inhibitor which acts specifically on carbonic
anhydrase. It is indicated in the treatment of :
i) Glaucoma: MOXAID Injection is useful in glaucoma (chronic simple (open angle)
glaucoma, secondary glaucoma and perioperatively in acute angle closure
glaucoma where delay of surgery is desired in order to lower intraocular pressure)
because it acts on inflow, decreasing the amount of aqueous secretion.
ii) Abnormal retention of fluids: MOXAID Injection is a diuretic whose effect is
due to the effect on the reversible hydration of carbon dioxide and dehydration
of carbonic acid reaction in the kidney. The result is a renal loss of HCO3- ion
which carries out sodium, water and potassium.
MOXAID Injection can be used in conjunction with other diuretics when effects
on several segments of the nephron are desirable in the treatment of fluid
retaining states.
iii) Epilepsy: In conjunction with other anticonvulsants best results with MOXAID
Injection have been seen in petit mal in children. Good results, however, have
been seen in patients, both children and adults, with other types of seizures
such as grand mal, mixed seizure patterns, myoclonic jerk patterns, etc.

Nothing of note to the prescriber.

6. PHARMACEUTICAL PARTICULARS
6.1 List of Excipients
Sodium hydroxide (for pH adjustment)
Hydrochloric acid (for pH adjustment)

6.2 Incompatibilities
None.

6.3 Shelf Life
24 months.

6.4 Special Precautions for Storage
Do not store above 25˚C.

6.5 Nature and Contents of Container
Glass vial with butyl rubber plug and aluminium ring seal.
Pack size: 500mg vial.

6.6 Instruction for Use, Handling and Disposal
Reconstitute each vial of MOXAID Injection with at least 5ml of water for injection
prior to use. The reconstituted solution is clear and colourless and does not contain
an antimicrobial preservative. Any unused solution must be stored in a refrigerator
and used within 24 hours. Any unused solution after this period must be discarded.
The direct intravenous route of administration is preferred. Intramuscular
injection may be employed but is painful due to the alkaline pH of the solution.

7. MARKETING AUTHORISATION HOLDER
Mercury Pharmaceuticals Ltd,
No.1 Croydon, 12-16 Addiscombe Road, Croydon CR0 0XT, UK

8. MARKETING AUTHORISATION NUMBER(S)
PL 12762/0219

9. DATE OF FIRST AUTHORISATION/RENEWAL OF AUTHORISATION
03/09/2012

10. DATE OF REVISION OF THE TEXT
September 2014
TN746
8533737 RA

HEALTH PROFESSIONALS’
USER LEAFLET

P151875

4.2. Posology and Method of Administration
Routes of Administration: Intravenous or intramuscular injection. The direct
intravenous route is preferred as intramuscular use is limited by the alkaline pH
of the solution.
i) Glaucoma (simple acute congestive and secondary):
Adults: 250 - 1000mg per 24 hours, usually in divided doses for amounts over
250mg daily.
ii) Abnormal retention of fluid: Congestive heart-failure, drug-induced oedema.
Adults: For diuresis, the starting dose is usually 250 - 375mg once daily in the
morning. If, after an initial response, the patient fails to continue to lose oedema
fluid, do not increase the dose but allow for kidney recovery by omitting a day.
Best results are often obtained on a regime of 250 - 375mg daily for two days,
rest a day, and repeat or merely giving MOXAID Injection every other day. The
use of MOXAID Injection does not eliminate the need for other therapy, e.g.
digitalis, bed rest and salt restriction in congestive heart failure and proper
supplementation with elements such as potassium in drug-induced oedema.
For cases of fluid retention associated with pre-menstrual tension, a daily dose
(single) of 125 - 375mg is suggested.

iii) Epilepsy
Adults: 250 - 1000mg daily in divided doses.
Children: 8 - 30mg/kg in daily divided doses and not to exceed 750mg/day.
The change from other medication to MOXAID Injection should be gradual.
Elderly: MOXAID Injection should only be used with particular caution in elderly
patients or those with potential obstruction in the urinary tract or with disorders
rendering their electrolyte balance precarious or with liver dysfunction.
For reconstitution please refer to section 6.6 below.

4.3 Contra-Indications
Moxaid Injection is contraindicated in situations in which sodium and/or
potassium blood levels are depressed, in cases of marked kidney and liver
dysfunction, suprarenal gland failure and hyper-chloremic acidosis. Moxaid
Injection should not be used in patients with hepatic cirrhosis as this may
increase the risk of hepatic encephalopathy.
Long-term administration of MOXAID Injection is contra-indicated in patients
with chronic non-congestive angle-closure glaucoma since it may permit
organic closure of the angle to occur while the worsening glaucoma is masked
by lower intraocular pressure.
MOXAID Injection should not be used in patients hypersensitive to
sulphonamides.

4.4 Special warnings and precautions for use
Suicidal ideation and behaviour have been reported in patients treated with
antiepileptic agents in several indications. A meta-analysis of randomised
placebo controlled trials of anti-epileptic drugs has also shown a small
increased risk of suicidal ideation and behaviour. The mechanism of this risk is
not known and the available data do not exclude the possibility of an increased
risk for MOXAID Injection.
Therefore patients should be monitored for signs of suicidal ideation and
behaviours and appropriate treatment should be considered. Patients (and
caregivers of patients) should be advised to seek medical advice should signs
of suicidal ideation or behaviour emerge.
Increasing the dose does not increase the diuresis and may increase the
incidence of drowsiness and/or paraesthesia.
Increasing the dose often results in a decrease in diuresis. Under certain
circumstances, however, very large doses have been given in conjunction with
other diuretics in order to secure diuresis in complete refractory failure.
When MOXAID Injection is prescribed for long-term therapy, special precautions
are advisable. The patient should be cautioned to report any unusual skin rash.
Periodic blood cell counts and electrolyte levels are recommended. Fatalities
have occurred, although rarely, due to severe reactions to sulphonamides. A
precipitous drop in formed blood cell elements or the appearance of toxic skin
manifestations should call for immediate cessation of MOXAID Inejction therapy.
In patients with pulmonary obstruction or emphysema where alveolar ventilation
may be impaired, MOXAID Injection which may aggravate acidosis, should be
used with caution.
In patients with a past history of renal calculi, benefit should be balanced against
the risks of precipitating further calculi.
The pH of parenteral acetazolamide is 9.1. Care should be taken during
intravenous administration of alkaline preparations to avoid extravasation and
possible development of skin necrosis.

4.5 Interactions with other Medicinal Products and other Forms of
Interaction
Acetazolomide is a sulphonamide derivative. Sulphonamides may potentiate the
effects of folic acid antagonists. Possible potentiation of the effects of folic acid
antagonists, hypoglycaemics and oral anti-coagulants. Concurrent
administration of acetazolamide and aspirin may result in severe acidosis and
increase central nervous system toxicity. Adjustments of dose may be required

when MOXAID Injection is given with cardiac glycosides or hypertensive agents.
When given concomitantly acetazolomide modifies the metabolism of phenytoin
leading to increased serum levels of phenytoin. Severe osteomalacia has been noted
in a few patients taking acetazolamide in combination with other anticonvulsants.
There have been isolated reports of reduced primidone and increased
carbamazepine serum levels with concurrent administration of acetazolamide.
Because of possible additive effects with other carbonic anhydrase inhibitors,
concomitant use is not advisable.

4.6 Pregnancy and Lactation
Acetazolamide has been reported to be teratogenic and embryotoxic in rats,
mice, hamsters and rabbits at oral or parenteral doses in excess of ten times
those recommended in human beings. Although there is no evidence of these
effects in human beings, there are no adequate and well-controlled studies in
pregnant women. Therefore, MOXAID Injection should not be used in
pregnancy, especially during the first trimester.
Acetazolamide has been detected in low levels in the milk of lactating women
who have been given MOXAID Injection. Although it is unlikely that this will lead
to any harmful effects in the infant, extreme caution should be exercised when
MOXAID Injection is administered to lactating women.

4.7 Effects on Ability to Drive and Use Machines
Increasing the dose does not increase the diuresis and may increase the
incidence of drowsiness and/or paraesthesia. Less commonly, fatigue, dizziness
and ataxia have been reported. Disorientation has been observed in a few
patients with oedema due to hepatic cirrhosis. Such cases should be under
close supervision. Transient myopia has been reported.
These conditions invariably subside upon diminution or discontinuance of the
medication.

4.8 Undesirable Effects
Adverse reactions during short-term therapy are usually non-serious. Those
effects which have been noted include: paraesthesia, particularly a tingling
feeling in the extremities, some loss of appetite; taste disturbance, polyuria,
flushing, thirst, headache, dizziness, fatigue, irritability, depression, reduced
libido and occasional instances of drowsiness and confusion. Rarely,
photosensitivity has been reported.
During long-term therapy, metabolic acidosis and electrolyte imbalance may
occasionally occur. This can usually be corrected by the administration of
bicarbonate.
Transient myopia has been reported. This condition invariably subsides upon
diminution or discontinuation of the medication.
Gastro-intestinal disturbances such as nausea, vomiting and diarrhoea.
Acetazolomide is a sulphonamide derivative and therefore some side effects
similar to those caused by sulphonamides have occasionally been reported.
These include fever, agranulocytosis, thrombocytopenia, thrombocytic purpura,
leukopenia and aplastic anaemia, bone marrow depression, pancytopenia, rash
(including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal
necrolysis), anaphylaxis, crystalluria, calculus formation, renal and ureteral colic
and renal lesions. Rarely, fulminant hepatic necrosis has been reported.
Other occasional adverse reactions include: urticaria, melaena, haematuria,
glycosuria, impaired hearing and tinnitus, abnormal liver function, renal failure
and, rarely, hepatitis or cholestatic jaundice, flaccid paralysis and convulsions.

Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal
product is important. It allows continued monitoring of the benefit/risk balance
of the medicinal product. Healthcare professionals are asked to report any
suspected adverse reactions via the Yellow Card Scheme at:
www.mhra.gov.uk/yellowcard.

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Source: Medicines and Healthcare Products Regulatory Agency

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