Name of Medicine
Pioglitazone hydrochloride.
Presentation
Pioglitazone 15mg, 30mg & 45mg tablets.
Key Practice Points
Therapeutic Indication:
- Treatment of type 2 diabetes where physical activity and dietary management has not resulted in adequate glycaemic targets.
https://www.pbs.gov.au/medicine/item/8694N-8695P-8696Q
Dose:
- Pioglitazone is taken once a day as a single dose with or without food.
- After starting (as with all glitazones) everyone should be monitored carefully for fluid retention. Oedema is reported more often in women. It is therefore suggested that the dose is started at 15 mg and be increased slowly, paying attention to any fluid retention.
- Monotherapy - The recommended dose of pioglitazone is 15 or 30 mg once daily, increasing after four weeks, to 45 mg once daily as required depending on glucose levels (person centre care).
- Dual and triple therapy - The recommended dose of Pioglitazone 30 mg once daily in combination with sulfonylureas, insulin, or metformin. If risk of hypoglycaemia, pioglitazone can be introduced at a dose of 15 mg. For those already on insulin, pioglitazone should be introduced at a dose of 15 mg once daily. Dosage can then be increased slowly.
- The dose of pioglitazone should not exceed 45 mg daily.
- Renal impairment - Dose adjustment in individuals with renal insufficient is not recommended. Those on dialysis should not take pioglitazone.
- Liver impairment - Pioglitazone should not be used in individuals with hepatic dysfunction.
Elderly:
- There is no need to adjust the dose in this cohort. However, due to the high incidence of bladder cancer, bone fracture and heart failure in this population, the benefits and risks should be considered carefully when considering its use.
Contraindications:
- Hypersensitivity to pioglitazone or any active ingredient
- Type 1 diabetes
- Individuals under the age of 18 years
- Pregnancy and lactation
- Cardiac failure or history of cardiac failure (New York Heart Association [NYHA] Class I, II, III or IV
- Bladder cancer or a history of bladder cancer
- Un-investigated macroscopic haematuria.
- Hepatic impairment.
Precautions:
- Bone Fractures - An increased incidence of bone fracture was noted in females taking rosiglitazone. The risk is also associated with men although it is suggested it is not as great.
- Eye Disorders - There is an increased risk of possibility of macular oedema.
- Increased risk of cardiac failure when rosiglitazone was added to treatment regimens that contained insulin or sulfonylureas. (annual cycle of care-cardiac screening, Diabetes MedsCheck referral back to GP for screening)
- Hypoglycaemia - Rosiglitazone in combination with insulin or oral hypoglycaemic agents that cause hypoglycaemia. may be at risk of increased low glucose levels (link to hypoglycaemia information). Encourage blood glucose monitoring and referral to appropriate health care professional for further advise on hypoglycaemia treatment. Consider Diabetes MedsCheck
- Oedema
- Weight gain (Diabetes MedsCheck, increase knowledge of how weight gain is occurring and referral pathway for help with healthy eating plan)
- Hypercholesterolemia (Diabetes MedsCheck, annual cycle of care, referral for cholesterol check, cholesterol monitoring in pharmacy)
- Bone fractures (monitoring for calcium and strong bones in pharmacy, referral pathways back to GP)
Adverse effects:
- Hypoglycaemia - Pioglitazone in combination with insulin or oral hypoglycaemic agents that cause hypoglycaemia. may be at risk of increased low glucose levels (link to hypoglycaemia information).Encourage blood glucose monitoring and referral to appropriate health care professional for further advise on hypoglycaemia treatment. Consider Diabetes MedsCheck
- Weight gain (Diabetes MedsCheck, increase knowledge of how weight gain is occurring and referral pathway for help with healthy eating plan).
- Oedema
- Bladder cancer (annual cycle of care-eye check, (Diabetes MedsCheck referral back to GP for screening)
- Increased appetite, dizziness, vertigo, flatulence, sweating, glycosuria, proteinuria and increased lactic dehydrogenase have been reported in combination with sulfonylurea. (Diabetes MedsCheck due to side effect profile).
- Hepatocellular dysfunction - There were reports of changes in liver enzymes post market. It is therefore recommended all individuals commenced on pioglitazone have liver enzymes checked before and during treatment. (Diabetes MedsCheck due to side effect profile).
Pharmacokinetic Properties - Summary
Absorption:
- Peak concentration is within two hours after oral administration from fasting state. food delays absorption slightly. Absolute bioavailability is approximately 83%.
Distribution:
- Pioglitazone is extensively bound to plasma protein >99%.
Metabolism:
- Pioglitazone undergoes extensive hepatic metabolism by cytochrome P450 2C8 and 3A4. Three of the six metabolites formed are active.
Excretion:
- After oral administration pioglitazone is found in faeces (55%) and urine (45%) The mean plasma elimination half-life of unchanged pioglitazone in humans is five to six hours and for its total active metabolites 16 to 23 hours.
For more detailed information on this product please consult the product information.
