pharm- midterm Flashcards
Which of the following progestins has the greatest anti- androgenic effect?
A. Norethindrone
B. Levonorgestrel
C. Cyproterone acetate
D. Drospirenone
C. Cyproterone acetate
mechanism of action of hormonal contraceptives
high estrogen and progesterone block GnRH release which block FSH and LH release
block LH reduced androgen production and increase SHBG
inhibit follicle development, ovulation, alter cervical mucus so sperm cant penetrate
absolute contraindications for progestin contraceptives
breast cancer
cerebrovascular disease
valvular heart disease
venous thromboembolism
diabetes with microvascular complications
pregnancy
uncontrolled hypertension
migraine with aura
liver cirrhosis
smoker >35 yrs old
how to choose an oral contraceptive
progrestins with anti-androgen for PCOS and acne
low estrogen if just for contraception
non-contraceptive benefits of OCPs
increase bone mineral density
decrease acne
decrease cancers
decrease peri-menopausal
decrease fibroids
adverse effects of OCPs
breakthrough bleeding/spotting, amenorrhea, nausea/vomiting, bloating, chloasma, breast tenderness, mood changes such as depression, headache
Major: thromboembolism (rare), stroke, retinal artery thrombosis, MI, benign liver tumor, cholelithiasis, hypertension.
danger signs if OCP has caused bad problem like stroke, hypertension, MI, liver tumor, thromboembolism
Watch for danger signals: ACHES—abdominal pain, chest pain, headaches, eye problems, severe leg pain
progestin only pills mechanism of action
inhibit the LH surge preventing ovulation, thicken cervical mucus, and decrease motility of an ovum in the fallopian tubes
indications for progestin only pils
patients over 35 years of age who smoke, cannot tolerate estrogen, have unwanted side effects with COCs (combined oral contraceptives), experience migraine headache with neurologic symptoms or are breastfeeding
adverse effects and CI of progestin only pill
ectopic pregnancy
contraindications:
**pregnacny and breast cancer
*viral hepatitis and liver tumors
1st and second generation progestins
norethrindone, norgestrel and levonorgestrel
norethrindone, norgestrel and levonorgestrel (1st and 2nd generation progestins) use
have high risk of metabolic side effects and higher androgenic activity
o Bad for PCOS, good for contraception
which progestin is best for anti-androgens
cyproterone acetate
followed by drsopirenone (4th generation)
risks with drospirenone (4th gen. progestin)
hyperkalemia, venous thromboembolism
2 emergency postcoital contraceptives
- levonorgestrel
- ulipristal acetate
1st line for hyperandrogenism (hisutims and acne) and for mentstural irregularity
combined oral contraceptives
insulin sensititizers mechanism of action in PCOS
- Reduce hyperinsulinemia and hyperandrogenemia
- Inhibit hepatic gluconeogenesis, reduce insulin and androgen, decrease LH-stimulated testosterone secretion
2 examples of insulin sensitizers
metformin
thiazolinediones (rosiglitazone and pioglitazone)
4 meds for hirsutism
spironolactone
finasteride
ovulation induction medications
aromatase inhibitors (letrozole and cloimphene citrate)
finasteride reduced
DHT
spironolactone inhibits _____. use with ______ because of
steroidogenesis; COC; teratogenic and alters menses
aromatase inhibitors (letrozole and clomiphene citrate) MOA
block conversion of androgen to estrogen
dysmenorrhea more common if
smokers
pain in dysnmernorrhea from
myometrial contractions via prostaglandins
1st choice for dysmenorrhea
oral contraception (if also want contraception) OR NSAIDS
Which of the following drugs can be used to induce ovulation in people with endometriosis?
A. Letrozole
B. Levonorgestrel
C. Elagolix
D. Leuprolide
A. Letrozole
NSAIDs to use for dysmenorrhea
- COX-2 inhibitors: celecoxib
- Non-selective- NSAIDs: ibuprofen, naproxen
acetaminophen is not as good for analgesic
when to take NSAIDs for dysmenorrhea
- Take when onset or symptoms or menses and continue on regular schedule for 2-3 days
NSAIDs inhibit
prostaglandins
progestin only contraceptive example to reduce blood loss
- Levonorgestrel intrauterine system (IUD)
contraindications for - Levonorgestrel intrauterine system (IUD)
: pregnancy, PID, postpartum endometriosis, uterine malignancies, cervicitis, liver disease
best option for endometrosisi
combined hormonal contraceptives
progestin only contraceptive in endometriosis
- Injectable medroxyprogesterone acetate or levonorgestrel IUS is more convenient than daily norethindrone
when to use opioid analgesics in endometrosis
if cant used NSAIDS
can be addicting
androgen agonist
danazol
androgen agonist for endometriosis
when not to use
danazol
- Endometriomas >1cm don’t respond well
adverse effects of androgen agonists
voice deepening, decrease breast size, increase weight, hirsutism, increase LDL, hot flashes, vaginal dryness
GnrH agonist name
elagolix, - - Leuprolide and goserelin
GnRH agonist in endometriosis
- As effective as COCs and progestins to manage endometriosis-associated pain
- But COCs have less side effects
what to do if using GnrH agonist
add back therapy (estrogen and progesterone)
bc can cause perimenospauseal sx like hot flashes, bone minders density, libido
ovulation induction example drug
letrozole
ovulation induction mechanism of action
inhibits aromatase enzyme; so cant convert to estrogen
o Reduces estrogen levels so pituitary makes more FSH for follicles
antifibrinolytic use and example
tranexamic acid for heavy periods
Which of the following drugs acts as an antagonist of leukotriene receptor interactions in target tissues?
A. Budesonide
B. Montelukast
C. Formoterol
D. Omalizumab
B. Montelukast
asthma defintion
- Inflammation of airways; activate mast cells to release bronchoconstrictors (histamine, leukotriene, prostaglandin) leads to smooth muscle contraction, vasodilation, mucus hypersecretion…
inhaled corticosteroids work on which receptor
- Increase b2 adrenergic receptor and antiinflam cytokines, decrease proinflam cytokines
how to reduce systemic exposure of inhaled corticosteroids on body
reduce systemic exposure via first past effect or prodrug that activated by lungs
o Ciclesonide is inert until activated by lung esterase’s
o Budesonide is metabolized by CYP3A4; bioavailability 10%
2 inhaled corticosteroids
ciclesonide
budesonide
use inhaled cortcosteroids with
bronchodilator
side effects of inhaled corticosteroids
: sore throat, dysphonia, oral thrush, decreased growth rate in kids, osteoperosis, glaucoma
inhaled beta2 agonist pathway
- Activate beta2 receptor activate adenylyl cyclase increase cAMP activate PKA muscle relaxation (via phosphorylation of contractile proteins) –> bronchodilation
side effects of inhaled beta2agonist
Tachycardia, palpitations, nervousness, tremor, hypokalemia, restlessness, dizziness, headache, nausea
short acting vs long acting inhaled beta2 agonist
short: salbutamol
long: salmeterol and formoterol
salbutamal (beta 2 agonist use)
use with daily inhaled cortocpsteroid
exercise induced asthma then use
beta 2 agonist before (i.e salbutamol)
anticholinergic bind
M3 muscarinic receptors to block cholinergic stimulation from vagus nerve
- Blocks calcium increase and prevents bronchoconstriction
anticholinergic examples long and short acting
short: ipatropium
long: tiotropium
use anticholinergic as
use as add on therapy to beta2-agonist for exacerbations or as an alternative if susceptible to tachycardia
leukotriene pathway for asthma -
- Asthma trigger (i.e. cold, antigens, exercise) release arachidonic acid which then is converted into leukotriene (LTA4) LTB4 and LTC4 LTC4 into LTD4 and LTE4 at target tissues (ie.. smooth muscle)
example of leukotriene antagonist
montelukast
montelukast use (leukotriene antagonist)
second line option add on
o Inhaled corticosteroid+ long acting beta agonist combo is better
o Might be more useful if have concomitant rhinitis
boxed warning for leukotriene receptor antagonist (montelukast)
neuropsychiatric effects i.e. depression, aggression, hallucinations, suicidal
biologics use
severe and uncontrolled asthma
types of biologics
IgE (omalizumab)
IL5 (eosinophil) (mepolizumab)
IL4/IL13 (dupilumab)
IGE neutralizing antibodies (biologic) exam and use
- Omalizumab
- For kids >6 yoa with IgE mediated asthma
interuleukin5 inhibitor (biologic) example and use
- Mepolizumab
- IL5 for eosinophils in allergies
- For kids >6 with eosinophilic asthma (via blood cell count)
IL4R neutralizing antibody (biologic) example and use
dupilumab
- IL4 and IL13 are inflammatory cytokines
- For kids >6 with severe asthma or atopic dermatitis
controller and reliever in asthma
Step 1-5
Controller: Low dose ICS- fomoteral as needed
Reliver: ICS- fomoteral, short acting beta2 agonist (as alternative)
asthma in pregnancy ; what to use and what not to use
- If uncontrolled can cause preterm birth, congenital anomalies, pre-eclampsia…
- Need good control
- Use inhaled corticosteroids and beta2-adrenergic receptor agonist same as above; safe
- Don’t use biologics
