Forxiga

Brand Name and Generics

Forxiga is the brand name for the medication known generically as dapagliflozin. It is a prescription medication used primarily in the treatment of type 2 diabetes mellitus and, in some instances, heart failure or chronic kidney disease.

Pharmacological Classification

Dapagliflozin falls under the class of medications called sodium-glucose co-transporter 2 (SGLT2) inhibitors. It works by blocking reabsorption of glucose in the kidneys, leading to excretion of glucose through urine.

Indications and Usage

Forxiga is indicated for adults with type 2 diabetes mellitus to improve glycemic control as an adjunct to diet and exercise. It’s also approved for use in reducing the risk of hospitalization for heart failure among patients with type 2 diabetes and established cardiovascular diseases or multiple cardiovascular risk factors. Moreover, it’s used to treat heart failure with reduced ejection fraction to reduce the risk of cardiovascular death and hospitalization for heart failure.

Dosage Forms and Strengths

Forxiga is available in tablet form in two strengths: 5 mg and 10 mg. Tablets are to be taken orally once daily, with or without food.

Dosing Recommendations

The recommended starting dose of Forxiga is 5 mg once daily, taken in the morning, with or without food. Depending on the efficacy and tolerability, the dose may be increased to 10 mg once daily.

Administration Instructions

Advise patients to swallow Forxiga tablets whole. Do not crush, split, or chew the tablets. Instruct patients to establish a routine for taking Forxiga at the same time each day to maintain a consistent level of medication in their system.

Therapeutic Mechanism of Action

Forxiga inhibits the SGLT2 protein found in the proximal renal tubules of the kidneys, which is responsible for the majority of glucose reabsorption. By inhibiting SGLT2, Forxiga increases the excretion of glucose in the urine, thereby lowering blood glucose levels.

Adjustment for Renal Impairment

In patients with moderate renal impairment (eGFR 45 to <60 mL/min/1.73 m^2), the maximum recommended dose of Forxiga is 5 mg once daily. It is not recommended for patients with an eGFR <45 mL/min/1.73 m^2, or in patients with end-stage renal disease (ESRD) who are on dialysis.

Important Pharmacokinetic Parameters

Forxiga has an oral bioavailability of approximately 78% and reaches peak plasma concentrations within 2 hours after dosing in the fasting state. The presence of food does not affect the overall bioavailability but may delay the time to peak concentration by about 1 hour. The medication demonstrates linear pharmacokinetics over the therapeutic dose range.

Metabolism and Elimination

Dapagliflozin is extensively metabolized primarily by UGT1A9 to inactive metabolites. The metabolites and unchanged dapagliflozin are excreted in urine and feces. The elimination half-life of dapagliflozin is approximately 12.9 hours.

Contraindications

Forxiga is contraindicated in patients with a history of serious hypersensitivity reactions to dapagliflozin or any of the components of Forxiga. It should not be used in patients with severe renal impairment, end-stage kidney disease, or in patients on dialysis.

Drug Interactions

Co-administration of Forxiga with diuretics or insulin and insulin analogs may increase the risk of hypotension and ketoacidosis. Adjustments in dosage of these medications may be necessary when initiating or changing the dose of Forxiga.

Specific Populations Considerations

Adjust dose for the elderly population based on renal function as they are more likely to have a decreased renal function. Assess renal function before initiating Forxiga and as clinically indicated. There are no adequate data on the use of Forxiga in pregnant women or nursing mothers; it should be used only if the potential benefit justifies the potential risk to the fetus or infant. The safety and effectiveness of Forxiga in pediatric patients have not been established.

Side Effects and Adverse Reactions

The most common side effects include urinary tract infections, genital mycotic infections, increases in urination, and thirst. Adverse reactions that may necessitate discontinuation include ketoacidosis, severe urinary tract infections, hypotension, acute kidney injury, and hypersensitivity reactions.

Monitoring Parameters

Monitor patients for signs and symptoms of metabolic acidosis, urinary tract infections, and genital infections. Regularly assess renal function, especially in patients with a history of renal impairment or those on medications that may impact renal function. Monitor blood pressure and lipid profiles as appropriate.

Overdosage Management

In the event of an overdose, initiate supportive treatment as dictated by the patient’s clinical status. Removal of dapagliflozin by hemodialysis has not been studied, and due to its high protein binding, it may not be effective.

Storage and Handling

Store Forxiga at room temperature, between 20°C to 25°C (68°F to 77°F). Keep the medication in the original container with the lid tightly closed and protect from moisture. Keep out of reach of children.

Patient Counseling Information

Counsel patients on the potential risks and benefits of Forxiga. Discuss the importance of adherence to dietary recommendations, regular exercise, and routine blood sugar monitoring. Inform patients about recognition and management of hypoglycemia, hyperglycemia, and complications such as dehydration and ketoacidosis. Advise patients to inform their healthcare provider of any other medications they may be taking and of any side effects that they experience.