Endocrine drugs ONLY Flashcards
NPH
Intermediate-acting insulin
Can be combined with short-acting insulin
Detemir
Long-acting insulin
Usually wears off during sleep
Glargine
Longest-acting insulin
No peak time of activity
Aspart
Short-acting insulin
Lispro
Short-acting insulin
Glulisine
Short-acting insulin
Metformin
Biguanide
Actions:
- Inhibits liver glucose production
- Sensitizes insulin receptors
- Reduces gut glucose absorption
AE:
- Dec. B12 and folate absorption
- Lactic acidosis w/ toxicity
- GI upset upon initiation
Drug of choice for initial therapy in type 2
Glipizide
Sulfonylurea
Actions: Promotes insulin release
AE:
- Hypoglycemia
- Weight gain
- Disulfiram reaction with alcohol
Glyburide
Sulfonylurea
Actions: Promotes insulin release
AE:
- Hypoglycemia
- Weight gain
- Disulfiram reaction with alcohol
Glinides
Meglitinide
Actions: Promotes insulin release
AE:
- Hypoglycemia
- Weight gain
Shorter acting than Sulfonylureas
Glitazones
Thiazolidinediones
Actions: Inc. insulin response from cell
AE:
- HF due to fluid retention
- Upper respiratory infections, headaches, sinusitis, myalgia
- Bladder carcinoma from long-term/high dose therapy
Acarbose
Alpha-glucosidase inhibitors
Actions: Inhibit brush border enzymes -> delayed carb absorption
AE:
- GI discomfort
- Dec. iron absorption -> anemia risk
- Long term -> liver dysfunction
Miglitol
Alpha-glucosidase inhibitors
Actions: Inhibit brush border enzymes -> delayed carb absorption
AE:
- GI discomfort
- Dec. iron absorption -> anemia risk
- Long term -> liver dysfunction
Dipeptidyl-peptidase-4 inhibitors (DDP-4)
Actions: Inc. incretin = inc. insulin secretion response
AE:
- Hypersensitivity reactions
- Rare: Pancreatitis
Sodium-glucose-2 transporter inhibitors (SGLT-2)
Actions: Block renal reabsorption of glucose -> glucose excreted in urine
AE:
- Female UTI
- Inc. urination -> dehydration, hypotension
Lugol solution
Class: Non-radioactive iodine
Uses: Hyperthyroidism
Actions: Inhibits T4/T3 synthesis and systemic release
AE: High doses can cause paradoxical response → hyperthyroid symptoms
Somatropin
Uses: Pediatric or adult GH deficiency
ROA: IM or subQ
Adverse effects: Hyperglycemia
Somatostatin
Uses: GH excess
Cabergoline
Class: Ergot alkaloid derivatives
- Dopamine agonists
Uses: Corrects amenorrhea, prolactin excess, and infertility
Actions: Activates dopamine receptors in anterior pituitary
- Inhibits prolactin secretion
AE: Headache, nausea, dizziness
Bromocriptine
Class: Ergot alkaloid derivatives
- Dopamine agonists
Uses: Corrects amenorrhea, prolactin excess, and infertility
Actions: Activates dopamine receptors in anterior pituitary
- Inhibits prolactin secretion
AE: Headache, nausea, dizziness
Tamoxifen
Class: SERMs
Actions:
- Inhbts. cell growth in breast tissue
- Protects against osteoporosis
- Improves lipid profile
AE:
- Inc. endometrial cancer risk
- Inc. hot flashes
- Inc. thromboembolism risk
Uses: Breast cancer prevention and treatment
Raloxifene
Class: SERMs
Actions:
- Inhbts. cell growth in breast tissue
- Protects against osteoporosis
- Improves lipid profile
AE:
- Inc. hot flashes
- Inc. thromboembolism risk
Uses:
- Osteo prevention
- Breast cancer prevention in high-risk patients
Combination oral contraceptives
Suppression of ovulation: high estrogen provides negative feedback to suppress FSH (follicle cannot mature, no ovulation occurs)
Also alters cervical mucus & endometrium
Excess estrogen: Nausea, breast tenderness, edema
Excess progestin: Inc. appetite, fatigue, depression
Progestin-only “minipills”
Cervical secretion changes
Depot medroxyprogesterone acetate
Actions: Inhibition of FSH/LH secretion
AE: Bone loss risk
Copper IUD
Actions: Local foreign body reaction and chemical changes that are toxic to sperm
AE: Pelvic inflammatory disease if STI is present
Levonorgestrel IUD
Actions: Thickens cervical mucus, inhibits ovulation, alters endometrium
AE: Pelvic inflammatory disease if STI is present
Mifepristone
Class: Antiprogestin
Uses: Medical abortion
Actions: Blocks progesterone receptors → de-implantation; cervical softening and dilation
AE:
- Abdominal pain
- Vaginal bleeding
- Bacterial infection (give antibiotic)
Contraindications: Ectopic pregnancy, hemorrhagic disorders, anticoagulant use
Misoprostol
Class: Prostaglandin
Uses: Medical abortion
Actions: Directly stimulates uterine contractions
AE:
- Abdominal pain
- Vaginal bleeding
- Bacterial infection (give antibiotic)
Contraindications: Ectopic pregnancy, hemorrhagic disorders, anticoagulant use
Clomiphene
Uses: Follicular maturation
Actions: Blocks estrogen receptors in the hypothalamus/pituitary
- Causes inc. in LH/FSH
- Blocks negative feedback so that follicular maturation and ovulation can occur
AE:
- Hot flashes
- Bloating
- Breast engorgement
- Ovarian hyperstimulation
Menotropin
Uses: Follicular maturation
Actions: 50:50 mix of LH:FSH, direct action on ovary to induce follicular maturation
- If ovaries can respond to LH/FSH, ovulation is ~100%
AE: Ovarian hyperstimulation
Follitropin
Uses: Follicular maturation
Actions: FSH that acts on ovary, stimulating follicles
AE: Ovarian hyperstimulation
hCG and choriogonadotropin alpha
Uses: Ovulation
Actions: Acts on ovary to induce ovulation by stimulating LH surge
- IM
- Administered AFTER clomiphene or menotropin/follitropins
AE: Ovarian hyperstimulation or rupture of ovarian cysts
Terbutaline
Class: B2 agonist
Actions: Agonizes B2 on uterine smooth muscle, dec. contractions
AE:
- Pulmonary edema
- HypoTN
- Hyperglycemia
- Tachycardia
Nifedipine
Class: Ca2+ channel blocker
Actions: Blocks Ca2+ from sarcoplasmic reticulum, dec. contractions
AE:
- Tachycardia
- Facial flushing
- Headache
- Dizziness
- Nausea
Indomethacin
Class: COX inhibitor
Actions: Inhibits PG synthesis, dec. contractions and cervical ripening
AE:
- Nausea
- Gastric irritation
- Inc. postpartum bleeding
Oxytocin receptor blockers
Block uterine contractions by preventing initiation
Magnesium sulfate
Class: ACh inhibitor
Uses: NOT A TOCOLYTIC
- Neuroprotective effects to fetus
Actions: Inhibits ACh at NMJ
AE:
- Adverse: HypoTN, flushing, headache, dizziness
- Severe: Hypothermia, paralytic ileus, pulmonary edema
Hydroxyprogesterase caproate
Uses: Prevention of preterm labor for singleton pregnancy/history of preterm labor
AE:
- Injection site reactivity
- Hives
- Nausea/diarrhea
Dinoprostone
Class: Prostaglandin (PGE2)
Actions: Cervical ripening via breakdown of collagenase
AE:
- Fetal distress
- Tachysystole
- Systemic absorption -> nausea/vomiting, diarrhea, fever
ROA: Vaginal gel or pouches
Pitocin/Oxytocin
Effects:
- Uterine stimulation: Inc. force, frequency and duration of contractions -> number of receptors inc. as labor progresses
- Milk ejection
- Water retention
AE:
- Shivering
- Temp elevation
Misoprostol (Cytotec)
Class: Prostaglandin
Uses: Postpartum hemorrhage
Actions: Stimulates uterine contractions
AE:
- Nausea/vomiting, diarrhea (rare)
- Shivering
- Temp elevation
Caboprost tromethamine (Hemabate)
Class: Prostaglandin
Uses: Postpartum hemorrhage
Actions: Stimulates uterine contractions and INTENSE vasoconstriction
Contraindications:
- Pelvic inflammatory disease
- Cardiac/pulmonary/renal disease
- Caution in asthma, HTN, diabetes
AE:
- GI issues
- HTN
- Bronchoconstriction
Methylergonovine (Methergine)
Uses: Postpartum hemorrhage
- Only in emergencies
Actions: Stimulates uterine contractions and arteriole/venous constriction
Contraindications/AE:
- HTN
- Nausea, vomiting
- Headache
Tranexamic acid (TXA)
Class: Fibrinolysis inhibitor
Uses: Menorrhagia
Actions: Inhibits plasmin
- Dec. fibrin mesh dissolving
- Keeps clots in the body
Contraindications/AE:
- History of thrombosis
Levothyroxine
Class: T4 replacement
Uses: Hypothyroidism
- Takes 1 month to take full effect
Contraindications/AE:
- Hyperthyroidism
~Affected by~
- Food (dec. absorption)
- CYP450 inducers induce metabolism
- Dec. T4 -> T3 metabolism
- Inc. thyroglobulin binding (binds T3 and T4 together)
- Warfarin: Inc. blood-thinning effects
- Catecholamines: Inc. sensitization of heart
ROA: PO (on empty stomach) and IV
Liothyronine
Class: T3 replacement
Uses: Hypothyroidism
- Only when T4 can’t convert to T3 or myxedema coma
Methimazole
Class: Thionamides
Uses: Hyperthyroidism
Actions: Inhibits peroxidase to inhibit T4/T3 synthesis
AE:
- Cannot be used in 1st trimester pregnancy, crosses too much into placenta
- Rare: agranulocytosis, hepatotoxicity, vasculitis
- Overdose: hypothyroidism
- Goiter bc no negative feedback to TSH → release more so enlarge gland
Propylthiouracil (PTU)
Class: Thionamides
Uses: Hyperthyroidism and thyrotoxic crisis
Actions: Inhibits peroxidase to inhibit T4/T3 synthesis peripherally
AE:
- Rare: agranulocytosis, hepatotoxicity, vasculitis
- Overdose: hypothyroidism
- Goiter bc no negative feedback to TSH → release more so enlarge gland
Spironolactone
Class:
- K+ sparing diuretic
- Aldosterone antagonist
Actions:
- Corrects HTN -> allows Na and water excretion
- Conserves K+ because hyper-aldosterone caused hypokalemia
AE:
- Hyperkalemia
- Gynecomastia
- Menstrual irregularities
Hydrocortisone
Identical to cortisol
Class: Glucocorticoid drug
Uses: Primary adrenal insufficiency (Addison’s disease)
Actions: Glucocorticoid and mineralcorticoid actions
AE: None at physiologic dose
ROA: PO, IV for stress dose
Dexmethasone
Class: Glucocorticoid drug
Uses: Secondary and tertiary adrenal insufficiency
Actions:
- High glucocorticoid activity
- Very little mineralocorticoid actions
Vasopressin
Uses: Diabetes insipidus and post-op abdominal distension
Effects: Vasoconstriction, identical to ADH
AE: All due to water intoxication/dec. osmolality
- Early signs: Drowsiness, confusion, headache
- Late signs: Seizures, coma
High vasopressin doses -> hypertension, angina, MI
Desmopressin (DDAVP)
Uses: Diabetes insipidus
Effects: Structurally analogous to ADH
AE: All due to water intoxication/dec. osmolality
- Early signs: Drowsiness, confusion, headache
- Late signs: Seizures, coma
ROA: PO, intranasal
No vasoconstriciton
Long duration
Prednisone
Class: Glucocorticoid drug
Uses: General adrenocortical insufficiency
Actions:
- Glucocorticoid activity
- Less mineralocorticoid activity
- Longest acting (more potent)
Subdermal etonogestrel implant
Progestin only
AE: Progestin side effects, irregular vaginal bleeding
Testosterone enanthate
Testosterone esters
Cause hepatotoxicity
AE: HEPATOTOXICITY, VIRILIZATION, prem epiphyseal plate closure, inc LDL, dec HDL, edema
Testosterone cypionate
Testosterone esters
Cause hepatotoxicity
AE: HEPATOTOXICITY, VIRILIZATION, prem epiphyseal plate closure, inc LDL, dec HDL, edema
Methyltestosterone
17-alpha-alkylated compounds
Cause hepatotoxicity
AE: HEPATOTOXICITY, VIRILIZATION, prem epiphyseal plate closure, inc LDL, dec HDL, edema
17-a abuse AE: HTN, suppressed LH/FSH, CAD/MI risk, aggressiveness
Sildenafil
Preferred
Oral PDE5 inhibitors
Actions: Inhibit PDE5 → cGMP accum → erection
AE: Hypotension, CANNOT TAKE w/ alpha block
Contraindications: MI, angina, hypotension, HF
Vardenafil
Prolonged QT
Oral PDE5 inhibitors
Actions: Inhibit PDE5 → cGMP accum → erection
AE: Hypotension, CANNOT TAKE w/ alpha block
Contraindications: MI, angina, hypotension, HF
Tadalafil
Long-acting
Oral PDE5 inhibitors
Actions: Inhibit PDE5 → cGMP accum → erection
AE: Hypotension, CANNOT TAKE w/ alpha block
Contraindications: MI, angina, hypotension, HF
Avanafil
Short-acting
Oral PDE5 inhibitors
Actions: Inhibit PDE5 → cGMP accum → erection
AE: Hypotension, CANNOT TAKE w/ alpha block
Contraindications: MI, angina, hypotension, HF
Finasteride
5-alpha reductase inhibitors
Uses: BPH
Action: inhibit T → DHT conversion + promote regression
AE: dec libido, gynecomastia, dec PSA → eval for prostate cancer
Dutasteride
5-alpha reductase inhibitors
Uses: BPH
Action: inhibit T → DHT conversion + promote regression
AE: dec libido, gynecomastia, dec PSA → eval for prostate cancer
Silodosin / Tamsulosin
Uses: BPH
Relaxes smooth muscle in bladder neck + prostate
Dec dynamic obst
AE: abnormal ejaculation
Doxazosin / Terazosin
Uses: BPH
Relaxes smooth muscle in bladder neck + prostate
AE: hypotension, dizziness, nasal congestion
