Elimination of drospirenone is virtually complete 10 days after the last dose. Chemistry
Drospirenone, also known as 1,2-dihydrospirorenone or as 17β-hydroxy-6β,7β:15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid, γ-lactone, is a synthetic steroidal 17α-spirolactone, or more simply a spirolactone. It is an analogue of other spirolactones like spironolactone, canrenone, and spirorenone. Drospirenone differs structurally from spironolactone only in that the C7α acetylthio substitution of spironolactone has been removed and two methylene groups have been substituted in at the C6β–7β and C15β–16β positions.Spirolactones like drospirenone and spironolactone are derivatives of progesterone, which likewise has progestogenic and antimineralocorticoid activity. The loss of the C7α acetylthio group of spironolactone, a compound with negligible progestogenic activity, appears to be involved in the restoration of progestogenic activity in drospirenone, as SC-5233, the analogue of spironolactone without a C7α substitution, has potent progestogenic activity similarly to drospirenone. History
Drospirenone was patented in 1976 and introduced for medical use in 2000. Schering AG of Germany has been granted several patents on the production of drospirenone, including WIPO and US patents, granted in 1998 and 2000, respectively. It was introduced for medical use in combination with ethinylestradiol as a combined birth control pill in 2000. Drospirenone is sometimes described as a "fourth-generation" progestin based on its time of introduction. The medication was approved for use in menopausal hormone therapy in combination with estradiol in 2005. Drospirenone was introduced for use as a progestogen-only birth control pill in 2019. A combined birth control pill containing estetrol and drospirenone was approved in 2021.
The maximum infusion rate for Cleviprex is 32 mg/hour. Most patients in clinical trials were treated with doses of 16 mg/hour or less. Because of lipid load restrictions, no more than 1000 mL (or an average of 21 mg/hour) of Cleviprex infusion is recommended per 24 hours. In clinical studies, no significant changes occurred in serum triglyceride levels in the Cleviprex treated patients. There is little experience with infusion durations beyond 72 hours at any dose. The infusion can be reduced or discontinued to achieve desired blood pressure while appropriate oral therapy is established. Safety information
Cleviprex is intended for intravenous use. Titrate drug depending on the response of the individual patient to achieve the desired blood pressure reduction. Monitor blood pressure and heart rate continually during infusion, and then until vital signs are stable. Patients who receive prolonged Cleviprex infusions and are not transitioned to other antihypertensive therapies should be monitored for the possibility of rebound hypertension for at least 8 hours after the infusion is stopped. In clinical trials, the safety profile of clevidipine was generally similar to sodium nitroprusside, nitroglycerin, or nicardipine in patients undergoing cardiac surgery.Cleviprex is contraindicated in patients with allergies to soybeans, soy products, eggs, or egg products; defective lipid metabolism such as pathologic hyperlipemia (rare genetic disorders characterized by abnormal triglyceride metabolism), lipoid nephrosis, or acute pancreatitis if it is accompanied by hyperlipidemia; and in patients with severe aortic stenosis. Hypotension and reflex tachycardia are potential consequences of rapid upward titration of Cleviprex.