drospirenone/ethinyl estradiol

Action and Spectrum

Actions and Spectrum 

A combined hormonal drug for birth control is drospirenone/ethinyl estradiol. It functions by blocking ovulation, thickening cervical mucus, and changing the uterine lining to stop a fertilised egg from implanting. 

drospirenone/ethinyl estradiol is primarily used as a contraceptive and has no antibacterial or antifungal characteristics according to its spectrum. Sexually transmitted infections cannot be treated or prevented with this substance. 

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Menstrual irregularities (4.7%) 

Abdominal pain/discomfort/tenderness (2.3%) 

Breast pain/discomfort/tenderness (8.3%) 

Mood changes, including affect lability, depression, alteration of mood, mood swings, and irritability (2.3%) 

Nausea/vomiting (4.5%) 

>10% 

Migraine/headache (10.7%) 

Premenstrual syndrome (13.2%) 

Frequency not defined 

Hypersensitivity 

Venous/arterial thromboembolic events, including intracardiac thrombosis, sagittal sinus thrombosis, DVT, stroke, intracranial venous sinus thrombosis, retinal vein thrombosis 

Toxic skin eruption 

Uterine leiomyoma 

Hyperkalemia 

Chloasma 

Irregular uterine bleeding 

Gallbladder disease 

Hypertension 

Black Box Warning

Black Box Warning 

The black box warning is in reference to the elevated risk of blood clots, which can result in life-threatening medical conditions like pulmonary embolism, heart attack or stroke. Compared to women who use alternative birth control methods, those who take drospirenone/ethinyl estradiol are at an increased risk of developing blood clots. 

According to the black box warning, women who smoke and are older than 35 should not use drospirenone/ethinyl estradiol due to the elevated risk of significant cardiovascular events. 

The warning also advices, avoiding using drospirenone/ethinyl estradiol in women who have a history of deep vein thrombosis, pulmonary embolism or specific clotting problems since they may increase the risk of blood clots. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Existing or potential pregnancy 
• History of blood clots, such as pulmonary embolism (PE) or deep vein thrombosis (DVT) 
• stroke or heart attack history 
• Breast cancer, or any other oestrogen- or progestin-sensitive malignancy, is either known or suspected. 
• liver tumours or liver illness 
• abnormal vaginal bleeding without diagnosis 

Caution: 

• women with diabetics 
• women with a history of aura-related migraines 
• Women who have previously experienced depression or other mental health issues 
• women who have experienced gallbladder illness in the past 
• women who have previously used hormonal contraceptives or who have a history of jaundice during pregnancy 
• women who have experienced hypertriglyceridemia 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A  

Lactation: Excretion into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology 

A synthetic progestin called drospirenone prevents ovulation and thickens cervical mucus to keep sperm from getting to the egg. It changes the uterine lining to stop a fertilized egg from implanting. 

drospirenone inhibits the effects of androgen hormones like testosterone since it has anti-androgenic action. Women may experience less acne and undesirable hair development as a result of this. 

In order to exert its effects, ethinyl estradiol, a synthetic version of estrogen, inhibits the release of the pituitary hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This stops the egg from developing and releasing from the ovaries. 

Pharmacodynamics 

The activities of the two active ingredients i.e., drospirenone and ethinyl estradiol are related to its pharmacodynamics. 

Inhibiting follicle-stimulating hormone (FSH) and luteinizing hormone (LH) secretion from the pituitary gland, ethinyl estradiol blocks follicle development and maturation, ovulation, and egg release. The decreases cervical mucus thickness and increases viscosity, making it challenging for sperm to reach the egg. 

drospirenone prevents the pituitary gland from secreting FSH and LH, which suppresses ovulation. It increases the cervical mucus viscosity to prevent sperm from accessing the egg and reduces the probability of implantation by altering the uterine lining. 

Pharmacokinetics 

Absorption   

Following oral administration, drospirenone/ ethinyl estradiol is quickly absorbed from the digestive tract. While drospirenone reaches its peak plasma concentration in 1 to 3 hours while ethinyl estradiol is under 1 to 2 hours. 

Distribution 

Both drospirenone and ethinyl estradiol have strong interactions with the plasma proteins albumin and sex hormone-binding globulin (SHBG), respectively. They are widely dispersed throughout the body, with the liver, kidney, and adrenal glands having the highest quantities. 

Metabolism 

The liver is where ethinyl estradiol and drospirenone are both metabolized. While drospirenone is primarily metabolized by the CYP3A4 and CYP2C19 pathways, ethinyl estradiol is primarily metabolized by the cytochrome P450 (CYP) 3A4 pathway. The metabolites are eliminated in the urine and feces. 

Elimination and excretion 

ethinyl estradiol has a half-life of around 24 hours in the body while drospirenone has a half-life of about 30 hours. The urine and feces are the primary excretion sites for the metabolites. 

Adminstartion

Administration:  

An oral tablet containing drospirenone/ethinyl estradiol is available and should be taken once daily.  

The tablets should be taken every day at the same time, with or without food. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: drospirenone/ethinyl estradiol 

Why do we use drospirenone/ethinyl estradiol? 

A combination hormonal contraceptive drug called drospirenone/ethinyl estradiol is used to prevent pregnancy.  

Other off-label use for drospirenone/ethinyl estradiol include treating excessive hair growth in women, management of excessive menstrual bleeding, pain relief for endometriosis-related pain in ovarian and endometrial cancer prevention in high-risk females.