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ACETAZOLAMIDE 500 MG POWDER FOR SOLUTION FOR INJECTION

Active substance(s): ACETAZOLAMIDE / ACETAZOLAMIDE

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Diamox® Sodium 500 mg
Powder for Solution for Injection

2879
04.05.17[P-3]

(acetazolamide)
PATIENT INFORMATION LEAFLET
Read all of this leaflet carefully before you start taking this medicine.
Keep this leaflet. You may need to read it again.
If you have any further questions, ask your doctor or pharmacist.
If any of the side effects become serious, or if you notice any side effects
not listed in this leaflet, please tell your doctor or pharmacist.
Your medicine is available using the above name but will be referred to as
Diamox Injection throughout this leaflet.
In this leaflet:
1. What Diamox Injection is and what it is used for
2. Before you are given Diamox Injection
3. How you are given Diamox Injection
4. Possible side effects
5. How to store Diamox Injection
6. Further information
1. WHAT DIAMOX INJECTION IS AND WHAT IT IS USED FOR
Diamox Injection contains the active substance Acetazolamide. This
belongs to a group of medicines known as carbonic anhydrase inhibitors.
Diamox Injection is used to treat:
- glaucoma (a condition of the eye), by reducing the pressure within the
eye.
- Fluid retention
- Some forms of epilepsy (“fits”), in combination with other anti-epileptic
drugs.
2. BEFORE YOU ARE GIVEN DIAMOX INJECTION
You should NOT be given Diamox Injection if:
- you know you are allergic to sulphonamides, sulphonamide derivatives
including acetazolamide or to any of the ingredients in the medicine
(listed in Section 6 at the end of this leaflet)
- you have, or have ever had severe liver disease (problems)
- You have, or have ever had severe kidney problems
- you have a particular type of glaucoma known as chronic non congestive
angle closure glaucoma (your doctor will be able to advise you)
- you have reduced function of the adrenal glands - glands above the
kidneys - (also known as Addison's disease)
- you have low blood levels of sodium and/or potassium or high blood levels
of chlorine (your doctor will advise you)
Speak to your doctor if any of the above applies to you.
Take special care and speak to your doctor before taking Diamox
Injection if:
- you have or have ever had kidney problems such as kidney stones
- you have lung problems such as chronic bronchitis or emphysema, which
causes difficulty in breathing
- you have diabetes or problems with your blood sugar level
- You are over the age of 65
A small number of people being treated with anti-epileptics such as
Diamox Injection have had thoughts of harming or killing themselves,
if at any time you have these thoughts, immediately contact your
doctor.
Taking other medicines:
Please tell your doctor or pharmacist if you are taking or have recently taken
any other medicines, including medicines obtained without a prescription.
The effects of any of these medicines may change, particularly if you are
taking, or using, any of the following:
- medicines for your heart such as cardiac glycosides (e.g. digoxin)
- medicines to reduce blood pressure
- medicines to thin your blood (e.g. warfarin)
- medicines to lower the sugar in your blood
- medicines for epilepsy or fits (in particular, phenytoin, primidone or
carbamazepine or topiramate)
- Drugs which interfere with folic acid, eg methotrexate, pyrimethamine, or
trimethoprim
- steroids such as prednisolone
- aspirin and related medicines, eg salicylic acid or choline salicylate for
mouth ulcers
- other drugs in the group of medicines called carbonic anhydrase inhibitors
- amphetamines (a stimulant), quinidine (treats an irregular heart beat),
methenamine (prevents urine infections) or lithium (treats severe mental
problems)
- sodium bicarbonate therapy
- ciclosporin (used to suppress the immune system)

Pregnancy and breast feeding:
Ask your doctor or pharmacist for advice before taking any medicines.
Diamox Injection SHOULD NOT be taken if you are pregnant, think you are
pregnant or are planning to become pregnant. It may be taken when breast
feeding but only on the advice of the doctor.
Driving and using machines:
If Diamox Injection makes you feel drowsy or confused you should not drive
or operate machines. Diamox Injection can occasionally cause shortsightedness; if this happens and you feel that you can no longer drive
safely, you should stop driving and contact your doctor.
Important information about some of the ingredients of Diamox
Injection:
This medicine contains less than 1 mmol sodium (23mg) per dose, i.e.
essentially “sodium-free”.
3. HOW YOU ARE GIVEN DIAMOX INJECTION
Diamox Injection is a white powder which will be dissolved in water to make
a solution for injection either into one of your veins (intravenous) or into one
of your muscles (intramuscular).
The dose varies from person to person depending on their condition. Your
doctor will decide on the most appropriate dose.
Before starting and during treatment your doctor will monitor your blood to
check that treatment with Diamox Injection is suitable for you.
If you are given more Diamox Injection than you should:
As the injection will be administered by a doctor, it is unlikely that you will be
given more than is necessary.
If you have any further questions on the use of this product ask your doctor.
4. POSSIBLE SIDE EFFECTS
Like all medicines, Diamox Injection can cause side effects, although not
everybody gets them.
All medicines can cause allergic reactions although serious allergic
reactions are very rare. Any sudden wheeziness, difficulty in
breathing, swelling of the eyelids, face or lips, rash or itching
(especially affecting your whole body) should be reported to a doctor
immediately.
Extremely rarely, Diamox Injection can affect the cells in your blood.
This could mean that you are more likely to catch infections and that your
blood may not clot properly. If you have a sore throat or fever or you notice
bruises or tiny red or purple spots on your skin you should contact your
doctor immediately. If your muscles feel weak or you have fits, you should
see your doctor immediately.
Common side effects include:
- headache
- diarrhoea
- feeling or being sick, loss of appetite, thirst, or a metallic taste in the
mouth
- dizziness, loss of full control of arms or legs
- looking flushed
- a need to pass urine more often than normal
- tiredness or irritability
- feeling over-excited
- a tingling or numbness in the fingers or toes, or coldness in the extremities
Other side effects include:
- depression
- drowsiness or confusion
- a loss of interest in sex
- ringing in the ears or difficulty in hearing
- temporary short-sightedness which subsides when the dosage is reduced
or treatment is stopped.
Rare cases of skin rashes including an increased sensitivity to sunlight
have been reported. If you experience any unusual skin rashes, inform your
doctor.
Very rarely, Diamox Injection can affect the liver and kidneys. If you
experience pain in your lower back, pain or burning when you pass urine,
have difficulty in passing urine, or you stop passing urine, have blood in your
urine, pale stools, or if your skin or eyes look slightly yellow, you should
contact your doctor. You should also contact your doctor if your stools are
black or tarry, or if you notice blood in your stools.
If you are given Diamox Injection for a long time it can occasionally affect
the amount of potassium, or sodium in your blood. Your doctor will probably
take blood tests to check that this does not happen. You might also
experience bone thinning or the risk of kidney stones with long-term therapy.
High or low blood sugar levels may occasionally occur.

If any of the side effects becomes serious, or if you notice any side
effects not listed in this leaflet, please tell your doctor or pharmacist.
Reporting of side effects:
If you get any side effects, talk to your doctor, pharmacist or nurse. This
includes any possible side effects not listed in this leaflet. You can also
report side effects directly via the Yellow Card Scheme at:
www.mhra.gov.uk/yellowcard.
By reporting side effects you can help provide more information on the
safety of this medicine.
5. HOW TO STORE DIAMOX INJECTION
Keep out of the sight and reach of children.
Do not store above 25°C.
Any unused solution can be stored in a refrigerator for up to 24 hours but
any unused solution after this period must be discarded.
Do not use after the expiry date. This date is printed on your pack.
The Expiry date refers to last day of that month.
For single use only.
If the powder becomes discoloured or show any other signs of deterioration,
consult your pharmacist who will tell you what to do.
Medicines should not be disposed of via wastewater or household waste.
Ask your pharmacist how to dispose of medicines no longer required.
These measures will help to protect the environment.
6. FURTHER INFORMATION
What Diamox Injection Contains:
The active substance is acetazolamide.
Each vial contains 500mg acetazolamide (as acetazolamide sodium).
What Diamox Injection looks like and contents of the pack:
Diamox Injection is a white powder, packed in a transparent glass vial with a
grey rubber stopper, aluminium ring seal and blue plastic plug. Before use, it
is made into a solution, using at least 5ml water for injection.
Each carton contains 1 vial.
MANUFACTURER AND PRODUCT LICENCE HOLDER
Manufactured by Mercury Pharmaceuticals Ltd., No. 1 Croydon,
12-16 Addiscombe Road, Croydon, CR0 0XT, United Kingdom.
Procured from within the EU by Product Licence holder:
Star Pharmaceuticals Ltd., 5 Sandridge Close, Harrow, Middlesex HA1 1XD.
Repackaged by Servipharm Ltd.
POM

PL 20636/2879

Leaflet revision and issue date (Ref) 04.05.17[P-3]
Diamox is a trademark of Wyeth Holdings LLC.

Blind or partially sighted?
Is this leaflet hard to see or read?
Call 020 8423 2111 to obtain the
leaflet in a format suitable for you.

HEALTH PROFESSIONALS’
USER LEAFLET

2879
04.05.17[H-3]

1. NAME OF THE MEDICINAL PRODUCT
Diamox Sodium 500mg Powder for Solution for Injection.
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Each vial contains 500 mg acetazolamide (as acetazolamide sodium).
For full list of excipients see section 6.1.
3. PHARMACEUTICAL FORM
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: Diamox 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: Diamox 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.
Diamox 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
Diamox 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.
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 Diamox injection
every other day. The use of Diamox 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 premenstrual 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 Diamox injection should be gradual.
Elderly: Diamox 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 to section 6.6 below
4.3 Contraindications
Diamox injection is contra-indicated 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. Diamox
injection should not be used in patients with hepatic cirrhosis as this may
increase the risk of hepatic encephalopathy.
Long-term administration of Diamox 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.
Diamox injection should not be used in patients hypersensitive to
sulphonamides.

4.4 Special warnings and special 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 Diamox 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 Diamox 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 occured, 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 Diamox injection therapy.
In patients with pulmonary obstruction or emphysema where alveolar
ventilation may be impaired, Diamox 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 Interaction with other medicinal products and other forms of
interaction
Acetazolamide 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 Diamox injection is given with cardiac
glycosides or hypertensive agents. When given concomitantly
Acetazolamide 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, Diamox 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 taken Diamox injection. Although it is unlikely that this
will lead to any harmful effects in the infant, extreme caution should be
exercised when Diamox 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.
Acetazolamide 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, leucopenia and aplastic anaemia, bone marrow
depression, pancytopenia, rash (including erythema multiforme, StevensJohnson 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.
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 Diamox 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
Nothing of note to the prescriber.
6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
None.
6.2 Incompatibilities
None.
6.3 Shelf life
60 months.
6.4 Special precautions for storage
Do not store above 25°C.
6.5 Nature and contents of container
Diamox Injection is a white powder, packed in a transparent glass vial with
a grey rubber stopper, aluminium ring seal and blue plastic plug. Before
use, it is made into a solution, using at least 5ml water for injection.
Each carton contains 1 vial.
6.6 Special precautions for disposal
Reconstitute each vial of Diamox 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 can be
stored in a refrigerator for up to 24 hours but 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. PRODUCT LICENCE HOLDER
Procured from within the EU by Product Licence holder:
Star Pharmaceuticals Ltd., 5 Sandridge Close, Harrow, Middlesex
HA1 1XD.
8. PRODUCT LICENCE NUMBER
PL 20636/2879
Leaflet revision and issue date (Ref): 04.05.17[H-3]

Acetazolamide 500 mg
Powder for Solution for Injection

2879
04.05.17[P-3]

PATIENT INFORMATION LEAFLET
Read all of this leaflet carefully before you start taking this medicine.
Keep this leaflet. You may need to read it again.
If you have any further questions, ask your doctor or pharmacist.
If any of the side effects become serious, or if you notice any side effects
not listed in this leaflet, please tell your doctor or pharmacist.
Your medicine is available using the above name but will be referred to as
Acetazolamide Injection throughout this leaflet.
In this leaflet:
1. What Acetazolamide Injection is and what it is used for
2. Before you are given Acetazolamide Injection
3. How you are given Acetazolamide Injection
4. Possible side effects
5. How to store Acetazolamide Injection
6. Further information
1. WHAT ACETAZOLAMIDE INJECTION IS AND WHAT IT IS USED FOR
Acetazolamide Injection contains the active substance Acetazolamide. This
belongs to a group of medicines known as carbonic anhydrase inhibitors.
Acetazolamide Injection is used to treat:
- glaucoma (a condition of the eye), by reducing the pressure within the
eye.
- Fluid retention
- Some forms of epilepsy (“fits”), in combination with other anti-epileptic
drugs.
2. BEFORE YOU ARE GIVEN ACETAZOLAMIDE INJECTION
You should NOT be given Acetazolamide Injection if:
- you know you are allergic to sulphonamides, sulphonamide derivatives
including acetazolamide or to any of the ingredients in the medicine
(listed in Section 6 at the end of this leaflet)
- you have, or have ever had severe liver disease (problems)
- You have, or have ever had severe kidney problems
- you have a particular type of glaucoma known as chronic non congestive
angle closure glaucoma (your doctor will be able to advise you)
- you have reduced function of the adrenal glands - glands above the
kidneys - (also known as Addison's disease)
- you have low blood levels of sodium and/or potassium or high blood levels
of chlorine (your doctor will advise you)
Speak to your doctor if any of the above applies to you.
Take special care and speak to your doctor before taking
Acetazolamide Injection if:
- you have or have ever had kidney problems such as kidney stones
- you have lung problems such as chronic bronchitis or emphysema, which
causes difficulty in breathing
- you have diabetes or problems with your blood sugar level
- You are over the age of 65
A small number of people being treated with anti-epileptics such as
Acetazolamide Injection have had thoughts of harming or killing
themselves, if at any time you have these thoughts, immediately
contact your doctor.
Taking other medicines:
Please tell your doctor or pharmacist if you are taking or have recently taken
any other medicines, including medicines obtained without a prescription.
The effects of any of these medicines may change, particularly if you are
taking, or using, any of the following:
- medicines for your heart such as cardiac glycosides (e.g. digoxin)
- medicines to reduce blood pressure
- medicines to thin your blood (e.g. warfarin)
- medicines to lower the sugar in your blood
- medicines for epilepsy or fits (in particular, phenytoin, primidone or
carbamazepine or topiramate)
- Drugs which interfere with folic acid, eg methotrexate, pyrimethamine, or
trimethoprim
- steroids such as prednisolone
- aspirin and related medicines, eg salicylic acid or choline salicylate for
mouth ulcers
- other drugs in the group of medicines called carbonic anhydrase inhibitors
- amphetamines (a stimulant), quinidine (treats an irregular heart beat),
methenamine (prevents urine infections) or lithium (treats severe mental
problems)
- sodium bicarbonate therapy
- ciclosporin (used to suppress the immune system)

Pregnancy and breast feeding:
Ask your doctor or pharmacist for advice before taking any medicines.
Acetazolamide Injection SHOULD NOT be taken if you are pregnant, think
you are pregnant or are planning to become pregnant. It may be taken when
breast feeding but only on the advice of the doctor.
Driving and using machines:
If Acetazolamide Injection makes you feel drowsy or confused you should
not drive or operate machines. Acetazolamide Injection can occasionally
cause short-sightedness; if this happens and you feel that you can no longer
drive safely, you should stop driving and contact your doctor.
Important information about some of the ingredients of Acetazolamide
Injection:
This medicine contains less than 1 mmol sodium (23mg) per dose, i.e.
essentially “sodium-free”.
3. HOW YOU ARE GIVEN ACETAZOLAMIDE INJECTION
Acetazolamide Injection is a white powder which will be dissolved in water to
make a solution for injection either into one of your veins (intravenous) or
into one of your muscles (intramuscular).
The dose varies from person to person depending on their condition. Your
doctor will decide on the most appropriate dose.
Before starting and during treatment your doctor will monitor your blood to
check that treatment with Acetazolamide Injection is suitable for you.
If you are given more Acetazolamide Injection than you should:
As the injection will be administered by a doctor, it is unlikely that you will be
given more than is necessary.
If you have any further questions on the use of this product ask your doctor.
4. POSSIBLE SIDE EFFECTS
Like all medicines, Acetazolamide Injection can cause side effects, although
not everybody gets them.
All medicines can cause allergic reactions although serious allergic
reactions are very rare. Any sudden wheeziness, difficulty in
breathing, swelling of the eyelids, face or lips, rash or itching
(especially affecting your whole body) should be reported to a doctor
immediately.
Extremely rarely, Acetazolamide Injection can affect the cells in your blood.
This could mean that you are more likely to catch infections and that your
blood may not clot properly. If you have a sore throat or fever or you notice
bruises or tiny red or purple spots on your skin you should contact your
doctor immediately. If your muscles feel weak or you have fits, you should
see your doctor immediately.
Common side effects include:
- headache
- diarrhoea
- feeling or being sick, loss of appetite, thirst, or a metallic taste in the
mouth
- dizziness, loss of full control of arms or legs
- looking flushed
- a need to pass urine more often than normal
- tiredness or irritability
- feeling over-excited
- a tingling or numbness in the fingers or toes, or coldness in the extremities
Other side effects include:
- depression
- drowsiness or confusion
- a loss of interest in sex
- ringing in the ears or difficulty in hearing
- temporary short-sightedness which subsides when the dosage is reduced
or treatment is stopped.
Rare cases of skin rashes including an increased sensitivity to sunlight
have been reported. If you experience any unusual skin rashes, inform your
doctor.
Very rarely, Acetazolamide Injection can affect the liver and kidneys. If you
experience pain in your lower back, pain or burning when you pass urine,
have difficulty in passing urine, or you stop passing urine, have blood in your
urine, pale stools, or if your skin or eyes look slightly yellow, you should
contact your doctor. You should also contact your doctor if your stools are
black or tarry, or if you notice blood in your stools.
If you are given Acetazolamide Injection for a long time it can occasionally
affect the amount of potassium, or sodium in your blood. Your doctor will
probably take blood tests to check that this does not happen. You might also
experience bone thinning or the risk of kidney stones with long-term therapy.
High or low blood sugar levels may occasionally occur.

If any of the side effects becomes serious, or if you notice any side
effects not listed in this leaflet, please tell your doctor or pharmacist.
Reporting of side effects:
If you get any side effects, talk to your doctor, pharmacist or nurse. This
includes any possible side effects not listed in this leaflet. You can also
report side effects directly via the Yellow Card Scheme at:
www.mhra.gov.uk/yellowcard.
By reporting side effects you can help provide more information on the
safety of this medicine.
5. HOW TO STORE ACETAZOLAMIDE INJECTION
Keep out of the sight and reach of children.
Do not store above 25°C.
Any unused solution can be stored in a refrigerator for up to 24 hours but
any unused solution after this period must be discarded.
Do not use after the expiry date. This date is printed on your pack.
The Expiry date refers to last day of that month.
For single use only.
If the powder becomes discoloured or show any other signs of deterioration,
consult your pharmacist who will tell you what to do.
Medicines should not be disposed of via wastewater or household waste.
Ask your pharmacist how to dispose of medicines no longer required.
These measures will help to protect the environment.
6. FURTHER INFORMATION
What Acetazolamide Injection Contains:
The active substance is acetazolamide.
Each vial contains 500mg acetazolamide (as acetazolamide sodium).
What Acetazolamide Injection looks like and contents of the pack:
Acetazolamide Injection is a white powder, packed in a transparent glass
vial with a grey rubber stopper, aluminium ring seal and blue plastic plug.
Before use, it is made into a solution, using at least 5ml water for injection.
Each carton contains 1 vial.
MANUFACTURER AND PRODUCT LICENCE HOLDER
Manufactured by Mercury Pharmaceuticals Ltd., No. 1 Croydon,
12-16 Addiscombe Road, Croydon, CR0 0XT, United Kingdom.
Procured from within the EU by Product Licence holder:
Star Pharmaceuticals Ltd., 5 Sandridge Close, Harrow, Middlesex HA1 1XD.
Repackaged by Servipharm Ltd.
POM

PL 20636/2879

Leaflet revision and issue date (Ref) 04.05.17[P-3]

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HEALTH PROFESSIONALS’
USER LEAFLET

2879
04.05.17[H-3]

1. NAME OF THE MEDICINAL PRODUCT
Acetazolamide 500mg Powder for Solution for Injection.
2. QUALITATIVE AND QUANTITATIVE COMPOSITION
Each vial contains 500 mg acetazolamide (as acetazolamide sodium).
For full list of excipients see section 6.1.
3. PHARMACEUTICAL FORM
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: Acetazolamide 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: Acetazolamide 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.
Acetazolamide 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
Acetazolamide 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.
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 Acetazolamide
injection every other day. The use of Acetazolamide 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 Acetazolamide injection should be
gradual.
Elderly: Acetazolamide 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 to section 6.6 below
4.3 Contraindications
Acetazolamide injection is contra-indicated 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. Acetazolamide injection should not be used in patients with
hepatic cirrhosis as this may increase the risk of hepatic encephalopathy.
Long-term administration of Acetazolamide 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.
Acetazolamide injection should not be used in patients hypersensitive to
sulphonamides.

4.4 Special warnings and special 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 Acetazolamide 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 Acetazolamide 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 occured, 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 Acetazolamide injection therapy.
In patients with pulmonary obstruction or emphysema where alveolar
ventilation may be impaired, Acetazolamide 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 Interaction with other medicinal products and other forms of
interaction
Acetazolamide 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 Acetazolamide injection is given with
cardiac glycosides or hypertensive agents. When given concomitantly
Acetazolamide 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, Acetazolamide 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 taken Acetazolamide injection. Although it is unlikely that
this will lead to any harmful effects in the infant, extreme caution should be
exercised when Acetazolamide 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.
Acetazolamide 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, leucopenia and aplastic anaemia, bone marrow
depression, pancytopenia, rash (including erythema multiforme, StevensJohnson 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.
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 Acetazolamide 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
Nothing of note to the prescriber.
6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
None.
6.2 Incompatibilities
None.
6.3 Shelf life
60 months.
6.4 Special precautions for storage
Do not store above 25°C.
6.5 Nature and contents of container
Acetazolamide Injection is a white powder, packed in a transparent glass
vial with a grey rubber stopper, aluminium ring seal and blue plastic plug.
Before use, it is made into a solution, using at least 5ml water for injection.
Each carton contains 1 vial.
6.6 Special precautions for disposal
Reconstitute each vial of Acetazolamide 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
can be stored in a refrigerator for up to 24 hours but 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. PRODUCT LICENCE HOLDER
Procured from within the EU by Product Licence holder:
Star Pharmaceuticals Ltd., 5 Sandridge Close, Harrow, Middlesex
HA1 1XD.
8. PRODUCT LICENCE NUMBER
PL 20636/2879
Leaflet revision and issue date (Ref): 04.05.17[H-3]

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Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

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