Contraception Pharmacology

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Questions and Answers

How do combination oral contraceptives primarily prevent pregnancy?

  • By directly killing sperm cells within the female reproductive tract.
  • By creating a physical barrier that prevents sperm from reaching the egg.
  • By increasing the thickness of the uterine lining to prevent implantation.
  • By inhibiting the secretion of LH and FSH, thereby preventing ovulation. (correct)

Which factor is most crucial when considering the use of progestin-only pills (POPs) for contraception?

  • POPs are more effective at preventing ovulation compared to combination pills.
  • POPs contain a higher dose of hormones, minimizing the risk of breakthrough bleeding.
  • POPs have a longer duration of action, providing protection even with missed doses.
  • POPs must be taken at precisely the same time each day to maintain efficacy. (correct)

What is the primary mechanism by which intrauterine devices (IUDs) containing levonorgestrel prevent pregnancy?

  • By forming a physical barrier that prevents the implantation of a fertilized egg.
  • By inducing a systemic hormonal surge that inhibits the release of the egg.
  • By creating a cytotoxic environment within the uterus that kills sperm cells.
  • By causing a chronic inflammatory response toxic to sperm and ova, and thickening cervical mucus. (correct)

Why is the timing of administration crucial for postcoital contraceptives like Plan B?

<p>To create a hostile uterine environment before implantation can occur. (A)</p> Signup and view all the answers

How do continuous dosage contraceptives like Lybrel function to prevent pregnancy?

<p>By providing a constant level of progestin and estrogen to suppress menstruation. (A)</p> Signup and view all the answers

What is the rationale behind using different amounts of estrogen and progestin in biphasic and triphasic oral contraceptives?

<p>To mimic the endogenous ratio of hormones during a menstrual cycle, reducing side effects. (C)</p> Signup and view all the answers

Why does the use of oral contraceptives in women over 35 who smoke present an increased risk of cardiovascular complications?

<p>The combination of smoking and estrogen increases the risk of thromboembolic events and myocardial infarction. (D)</p> Signup and view all the answers

How do hepatic enzyme inducers reduce the efficacy of oral contraceptives?

<p>By increasing the metabolism of estrogens and progestins, leading to decreased plasma concentrations. (C)</p> Signup and view all the answers

What is the potential effect of broad-spectrum antimicrobials on the efficacy of oral contraceptives, and why?

<p>Antimicrobials interfere with the enterohepatic cycling of estrogens by altering GI flora. (C)</p> Signup and view all the answers

Why might a progestin-only contraceptive method be preferred over a combined estrogen-progestin method in certain clinical scenarios?

<p>Progestin-only methods do not carry the same increased risk of thromboembolic events as combined methods. (D)</p> Signup and view all the answers

What critical aspect differentiates Seasonale from traditional monthly oral contraceptives?

<p>Seasonale involves an extended cycle of active pills followed by a shorter interval of inert pills. (B)</p> Signup and view all the answers

How might combination oral contraceptives reduce the risk of ovarian and endometrial cancers?

<p>By suppressing ovulation, they reduce the repeated trauma and cell proliferation in the ovaries and uterus. (B)</p> Signup and view all the answers

For which of the following conditions would combination oral contraceptives be absolutely contraindicated?

<p>Suspected breast cancer or other estrogen-dependent cancer. (B)</p> Signup and view all the answers

What is the significance of monitoring triglyceride levels in women using hormonal contraceptives?

<p>To assess the risk of cardiovascular events, as hormonal contraceptives can increase triglyceride levels. (A)</p> Signup and view all the answers

How does ethinyl estradiol, used in many oral contraceptives, differ from naturally occurring estradiol in terms of its metabolic stability?

<p>Ethinyl estradiol contains an ethinyl group that reduces first-pass metabolism, increasing its oral bioavailability. (B)</p> Signup and view all the answers

What specific characteristic of desogestrel makes it a unique progestin to use in oral contraceptives?

<p>It has minimal androgenic activity compared to other progestins. (B)</p> Signup and view all the answers

Why is the use of certain anticonvulsants a concern for women using hormonal contraceptives?

<p>Anticonvulsants increase the metabolism of estrogens and progestins, reducing contraceptive efficacy. (B)</p> Signup and view all the answers

What distinguishes drospirenone from other progestins used in oral contraceptives?

<p>It possesses antimineralocorticoid activity, potentially affecting potassium levels. (A)</p> Signup and view all the answers

What is the primary reason some adolescents are considered to have a relative contraindication for oral contraceptive use?

<p>Oral contraceptives can lead to premature closure of epiphyseal plates, stunting growth. (A)</p> Signup and view all the answers

What is the rationale behind using anti-emetics in conjunction with post-coital oral contraceptives?

<p>To counteract the common side effects of nausea and vomiting caused by high hormone doses. (D)</p> Signup and view all the answers

What are the long term effects of using progestin-only contraception on the endometrium?

<p>Leads to an atrophic endometrium (B)</p> Signup and view all the answers

Why are combination contraceptives not recommended for smokers over the age of 35?

<p>Due to an increased risk of cardiovascular adverse effects. (A)</p> Signup and view all the answers

What key factor determines that progestin only medication is given?

<p>When estrogens are contraindicated (A)</p> Signup and view all the answers

What is the efficacy dependance of Progestin only pills?

<p>Based on the time of day it is taken. (B)</p> Signup and view all the answers

What is the common ingredient usually found in Progestin-only preperations?

<p>Norethindrone (D)</p> Signup and view all the answers

Flashcards

Contraceptives: Primary Use

Primary use of estrogens and progestins in a clinical setting, delivered via pills, SC and IM injections, IUDs and implants.

Monophasic Oral Contraceptives

Oral contraceptives that deliver a constant amount of estrogen and progestin throughout the cycle.

Biphasic/Triphasic Oral Contraceptives

Oral contraceptives where estrogen and progestin levels vary during the cycle, mimicking the body's natural hormone fluctuations.

Seasonale

Oral contraceptive regimen with ethinyl estradiol/levonorgestrel taken for 84 days, followed by 7 days of inert tablets.

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Lybrel

Oral contraceptive with ethinyl estradiol/levonorgestrel taken continuously for 365 days to suppress menstruation.

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Combination Contraceptives: Mechanism

Contraceptives that inhibit LH and FSH secretion, suppress the midcycle LH surge, thicken cervical mucus, speed ovum transport, and make the endometrium less favorable for implantation.

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Progestin-Only Pills

Taken daily, contains norethindrone, does not suppress ovulation and leads to atrophic endometrium.

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Medroxyprogesterone acetate

Injected progestin-only contraception; lasts for 3 months.

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Etonogestrel

Inserted under the skin to provide contraception for up to 3 years, though it can cause menstrual irregularities.

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Intrauterine Device (IUD)

Device that releases levonorgestrel.

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Post-Coital Oral Contraceptives

Includes Plan A: 100-120 ug ethinyl estradiol/.5-.75mg levonorgestrel AND Plan B .75mg Levonorgestrel

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Cardiovascular Adverse Effects of Contraceptives

Includes increased risk of myocardial infarction, hypertension, and increased triglyceride levels.

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Thromboembolic Disease & Contraceptives

Contraceptives may increase risk of stroke by increasing levels of fibrinogen and coagulation factors, and decreasing antithrombin III levels.

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Reproductive Organ Effects

Reduced incidence of ovarian and endometrial cancers and reduced incidence of pelvic inflammatory disease.

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Hepatobiliary System Effects

Increased incidence of gallbladder disease and gallstones.

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Absolute Contraindications of Oral Contraceptives

Vascular diseases, being over 35 (especially if a smoker), liver disease, suspected breast cancer or estrogen-dependent cancer, and strong family history of breast cancer.

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Relative Contraindications of Oral Contraceptives

Hypertension, diabetes, migraines, convulsive disorder, undiagnosed menstrual bleeding/breast lumps and adolescents who have not completed bone fusion.

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Drug Interactions Reducing Efficacy of Contraceptives

Antimicrobials and hepatic enzyme inducers.

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Antimicrobials Interactions with Contraceptives

Antimicrobials decrease oral bioavailability by killing GI flora needed for enterohepatic cycling of estrogens.

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Hepatic Enzyme Inducers Interactions

Increase metabolism of estrogens and progestins.

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Monophasic Combinations

Constant amount of estrogen and progesterone.

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Biphasic/Triphasic combinations

Estrogen and progestin varies.

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Benefits of oral contraceptives

Ovarian cysts and cancer, Endometrial cancer, Benign breast disease (fibrocystic), Pelvic inflammatory disease, Premenstrual syndrome, Dysmenorrhea, Endometriosis, Acne, Hirsutism

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Contraceptive effect

Leads to atrophic endometrium impairing implantation. and Viscous cervical mucus

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Useful Progestin-Only

Especially useful for women in whom estrogens are contraindicated

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Study Notes

Class Overview

  • Contraception pharmacology includes discussion of:
    • Menstrual cycle
    • Combination contraceptives
    • Progestin-only methods
    • Intrauterine devices
    • Postcoital contraceptives

Contraceptives: General Information

  • Estrogens and progestins are primarily used in a clinical setting
  • Delivery Methods: pills, subcutaneous (SC) injections, intramuscular (IM) injections, intrauterine devices, and implants
  • Formulations contain a combination of estrogen and progestins, or progestin only

Oral Contraceptives: Combination Pills

  • Estrogen dosage ranges from 20-50 ug/day
    • Including ethinyl estradiol or mestranol, which is metabolized to ethinyl estradiol
  • Progestin dosage ranges from 0.05-2.5 mg/day
    • Including norethindrone, norgestrel, levonorgestrel, norethindrone acetate, ethynodiol diacetate, drospirenone, and desogestrel
  • Lower luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels lead to failure to ovulate

Oral Contraceptives: Mono, Bi, and Tri-Phasic

  • Monophasic Combinations:
    • Deliver a constant amount of estrogen and progesterone
    • Involve 21 days of active pills followed by 7 days of inert tablets to induce menses
    • Formulations can vary in the amounts of estrogen and progestin
  • Biphasic/Triphasic Combinations
    • Estrogen and progestin levels vary
    • Mimic the endogenous ratio of hormones
    • 21 days of active pills are followed by 7 days of inert tablets to induce menses

Oral Contraceptives: Continuous Dosage

  • Seasonale:
    • Contains ethinyl estradiol/levonorgestrel
    • Taken for 84 days, followed by 7 days of inert tablets
    • This results in 4 menses per year
  • Lybrel:
    • Contains ethinyl estradiol/levonorgestrel
    • Constant dosing for 365 days, which suppresses menses

Combination Contraceptives: Mechanism of Action

  • Inhibit LH and FSH secretion through feedback inhibition
  • Suppress the midcycle LH surge needed for ovulation
  • Impact the genital tract:
    • Causes the thickening of cervical mucus
    • Increases the speed of ovum transport
    • Makes the endometrium less favorable for implantation

Progestin-Only Preparations

  • Primarily contain norethindrone
  • Taken daily and continuously
  • Ovulation is typically not suppressed
  • Less effective than combination therapy
  • Contraceptive effect is unclear
    • May lead to atrophic endometrium impairing implantation
    • Increases viscosity of cervical mucus
  • Abnormal menstrual bleeding can occur in 25% of users
  • It is especially useful for women where estrogens are contraindicated due to health concerns

Progestin-Only Preparations: Specific Formulations

  • Medroxyprogesterone Acetate:
    • Administered via subcutaneous or intramuscular injections
    • Provides contraception for 3 months
  • Etonogestrel:
    • Inserted as a single rod under the skin
    • Contraception for 3 years
    • Can result in menstrual and bleeding irregularities
  • Intrauterine Devices:
    • Contain levonorgestrel

Post-Coital Oral Contraceptives

  • Plan A:
    • Contains 100-120 ug ethinyl estradiol/0.5-0.75 mg levonorgestrel at higher doses
    • Effective if treatment begins within 72 hours of coitus
  • Plan B:
    • Contains 0.75 mg levonorgestrel
    • Effective if started within 72 hours of coitus
  • Nausea and vomiting are common, and anti-emetics are often combined
  • Contraindicated in confirmed pregnancy

Adverse Effects of Contraceptives: Cardiovascular

  • Increased risk of morbidity and mortality due to myocardial infarction
  • Can cause hypertension
  • Increased levels of triglycerides
  • Women over 35 have a heightened risk of cardiovascular complications

Adverse Effects of Contraceptives: Thromboembolic and Reproductive

  • Thromboembolic Disease:
    • Increased risk of stroke
      • Due to fibrinogen and coagulation factors increases, antithrombin III levels are decreased
  • Reproductive Organs:
    • Reduced incidence of ovarian and endometrial cancers
    • Reduced incidence of pelvic inflammatory disease

Adverse Effects of Contraceptives: Other

  • Hepatobiliary System:
    • Increased incidence of gallbladder disease and gallstones
  • Others:
    • weight gain, edema, breast tenderness, headache, mood alteration, and spotting

Contraindications of Oral Contraceptives

  • Absolute Contraindications:
    • Vascular diseases
    • Age over 35, particularly if the woman is a smoker
    • Liver disease
    • Suspected breast cancer or other estrogen-dependent cancer
    • A strong family history of breast cancer
  • Relative Contraindications:
    • Hypertension
    • Diabetes
    • Migraines
    • Convulsive disorder
    • Undiagnosed menstrual bleeding
    • Undiagnosed breast lumps
    • Adolescents who have not completed bone fusion

Benefits of Oral Contraceptives

  • Reduced Risk:
    • Lower dose combinations lead to lower risk.
      • Ovarian cysts and cancer
      • Endometrial cancer
      • Benign breast disease (fibrocystic)
      • Pelvic inflammatory disease
  • Improvements:
    • Premenstrual syndrome
    • Dysmenorrhea
    • Endometriosis
    • Acne
    • Hirsutism

Drug interactions that reduce the Efficacy

  • Antimicrobials:
    • Decrease oral bioavailability by killing the GI flora needed for enterohepatic cycling of estrogens
  • Hepatic enzyme inducers increase the metabolism of estrogens and progestins:
    • Anticonvulsants
    • Phenytoin
    • Barbiturates
    • Carbamazepine
    • Ethosuximide
    • Rifampin
    • Griseofulvin

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