Lecture 19 - Oral Contraceptives

Front 1

Which oral contraceptive has the fewest contraindications

Back 1

Progesterone only pill

Front 2

Progesterone only pills only downfall is that

Back 2

You have to maintain rigid compliance.

Front 3

The combination pill contains which two components

Back 3

an estrogen and a progesterone.

Front 4

AVA30ED is an example of

Back 4

Combination pill - contains levongesterol and ethinylestradiol.

Front 5

List 3 minor side effects of the combination pill

Back 5

Weight gain

Acne

Hair Growth

Front 6

The biggest risk when on the COC is

Back 6

Deep Vein Thrombosis

Front 7

Risk factors for DVT especially when combined with COC;

Back 7

Smoking

Older ages

Family History of DVT

Hypertension

Heart Disease

Prolonged immobilisation

Front 8

Lifetime exposure to estradiol is a risk factor for

Back 8

Breast Cancer

Front 9

Which two cancers are prevalent in those on COC

Back 9

Liver and Breast

Front 10

Excess risk of breast cancer dissipates how long after stopping the COC

Back 10

10 years :O

Front 11

Why is COC linked to breast cancer?

Back 11

Estrogen is a carcinogen so increases the risk of developing cancer

Estrogen also signals breast cancer cells (which are positive for the estrogen receptor) to divide so stimulates the growth of existing cancer.

Front 12

Apoptosis occurs in which stage of the cell cycle?

Back 12

G2 phase

Front 13

DNA replication occurs in which stage of the cell cycle?

Back 13

The S Phase.

Front 14

Cell division occurs in which phase of the cell cycle?

Back 14

M-phase

Front 15

The function of the G2 phase of cell division is primarily

Back 15

Repair of damaged DNA or apoptosis of the cells which are too damaged.

Front 16

The effect of estrogen on the G2 phase of cell division

Back 16

Estrogen mosulates the genes responsible for DNA repair ultimately reslting in a decrease in the effectiveness of the G2 phase (repair) of the cell therefore damaged cells are able to replicate

Front 17

DNA mutations occur in which phase of the cell cycle?

Back 17

S-Phase

Front 18

The estrogen receptor is what kind of receptor?

Back 18

Nuclear receptor

Front 19

Phase I Metabolism of Estrogen:

Back 19

Metabolised by CYP3A4 in the liver

Front 20

Phase II metabolism of Estrogen:

Back 20

Conjugated with glucuronide and sulfate in the liver

Front 21

Drug Interactions of COC

Inducers of CYP3A4

Back 21

Drugs that Induce CP3A4 cause decreased drug effectiveness.

- St Johns wort

- Barbituates

- Griseofulvin (antifungal)

- Rifampin (antibiotic)

- Carbamazpine

- Phenytoin

- Epilepsy medications

Use barrier method during drug administratio and for 28 days afterwards

Front 22

Drug interactions of COC

Inhibitors of CYP3A4

Back 22

Cause decreased estrorgen metabolism and increase side effects:

Erythromycin - antibiotic

Front 23

Drugs that modulate estrogen excretion

Back 23

Penecillins and Tetracyclines.

Inhibit the enzyme Beta-Glucuronidase and estrogen is excreted.

Use barrier method during drug course and 7 days after completion.

Front 24

Induction of CYP3A4 is via

Back 24

Nuclear receptor mechanism

RXR (retinoid X receptor) and PXR (pregnane X receptor)

Results in an increase in protein expression

Front 25

2 methods of CYP3A inhibition

Back 25

Competitive inhibition

Destruction of the enzyme

Front 26

Patients on Roaccutane:

A. MUST NOT take contraception

B. MUST take contraception

Back 26

B - Roaccutane is a potent teratogen so indivicuals taking it should NOT become pregnant.

Front 27

Grapefruit:

A: Induces CYP3A4

B: Induces CYP2E1

C: Inhibits CYP3A4

Back 27

C

Front 28

Induction of CYP3A4 enzymes will INCREASE/DECREASE the effect of COC?

Back 28

Decrease as Estrogen is metabolised by CYP3A4 so induction of CYP3A4 will reduce the amount of estrogen in the plasma.

Front 29

Inhibition of CYP3A4 will DECREASE/INCREASE the effect of COC?

Back 29

Increase.