Natsumi Pharm - Endo Flashcards
Mineralocorticoid & Glucocorticoid
PREGNENOLONE
precursor of progestogens, mineralocorticoids, glucocorticoids, androgens, and estrogens
Fludrocortisone
Mineralocorticoid
Prednisone Dexamethasone Hydrocortisone Fluticasone Methylprednisolone Mometasone Triamcinolone Clobetasol propionate Prednisolone Beclomethasone Budesonide Fluocinonide
Glucocorticoid
Pills, Oral/nasal, or topica?
Dexamethasone Prednisone Methylprednisolone Prednisolone Fluticasone Mometasone Beclomethasone Budesonide Clobetasol propionate Fluocinonide Mometasone Fluticasone Triamcinolone Hydrocortisone
Pills Dexamethasone Prednisone Methylprednisolone Prednisolone
Oral/Nasal sprays Fluticasone Mometasone Beclomethasone Budesonide
Topicals Clobetasol propionate Fluocinonide Mometasone Fluticasone Triamcinolone Hydrocortisone
Estrone (E1)
marker post-menopause (stored in adipose) and for cancer (ovary, testes, adrenals)
Estradiol (E2)
most prevalent outside of pregnancy
Estriol (E3), considered “protective”—highest in pregnancy
Estriol (E3)
considered “protective”—highest in pregnancy
Ethinyl estradiol
The only estrogen used in oral contraceptive pills
Lowest effective dose of ethinyl estradiol preferred to reduce risk of DVT
Conjugated estrogens
Vaginal cream is Estrace
Pregnancy category X—no reason to use in a pregnant woman
Medroxyprogesterone acetate
Progesterone
Uses: prevention of endometrial hyperplasia in nonhysterectomized postmenopausal women who are receiving conjugated estrogens tablets; secondary amenorrhea; abnormal uterine bleeding (fibroids)
Bloating symptoms, migraine, weight change
Contraindicated in women with undiagnosed abnormal genital bleeding; known, suspected, or history of breast cancer; known or suspected estrogen- or progesterone-dependent neoplasia; active DVT, PE, or a history of these conditions; active arterial thromboembolic disease (for example, stroke and MI), or a history of these conditions; known liver impairment or disease; known or suspected pregnancy.
WARNINGS: cardiovascular disorders, breast cancer, probably dementia
Pregnancy category X (natural progesterone suppositories are sometimes used in the first trimester to help hold a pregnancy in a woman who has miscarried previously)
Levonorgestrel
Progestin
Mirena/Skyla/Kyleena (IUD); Plan B/My Way/Next Choice (“morning after” pill, 1.5mg); Norgeston (“mini”-pill 0.03mg/progestin-only birth control pill)
Norethindrone
Used alone or in combination with ethinyl estradiol for combination (progestin + estrogen) oral contraceptive and menopausal agent (norethindrone + EE)
Pregnancy category X
Drospirenone
Used in combination with ethinyl estradiol for combination oral contraception
Contraindicated in smokers, particularly over age 35 years; associated with increase in gall bladder disease
Pregnancy category X
Norgestimate
Used in combination with ethinyl estradiol for combination oral contraception
Contraindicated in smokers, particularly over age 35 years; associated with increase in gall bladder disease
Pregnancy category X
Norelgestromin
Used in combination with ethinyl estradiol for combination oral contraception
Contraindicated in smokers, particularly over age 35 years; associated with increase in gall bladder disease
Pregnancy category X
5 letter = pathch NOR EL GE STRO MIN (5 syllable)
OCP’s nutrient depletion
Folic acid B1, B2, B3 (variable), B6, B12 Vitamin C Calcium Magnesium Selenium Zinc Tyrosine
Drospirenone/ethinyl estradiol
Norethindrone/ethinyl estradiol
Norgestimate/ethinyl estradiol
OCP
Black box warning: stroke, MI, PE, DVT, breast cancer, dementia
Clomiphene
Ovulatory stimulant
Uses: treatment of ovulatory dysfunction in women desiring pregnancy after impediments to achieving pregnancy have been excluded or adequately treated
Best outcomes seen in women with polycystic ovary syndrome, amenorrhea-galactorrhea syndrome, psychogenic amenorrhea, post-oral-contraceptive amenorrhea, and certain cases of secondary amenorrhea of undetermined etiology.
Warnings: potential for ovarian hyper-stimulation syndrome and hepatic dysfunction.
Pregnancy category X
Dehydroepiandrosterone (DHEA)
Testosterone
Androgen
(DHEA is a prescriptive agent—as is Melatonin—elsewhere in the world; here in the US, both are available over-the-counter.)
Testosterone
Used for: primary hypogonadism (congenital or acquired)-testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome; or orchidectomy; hypogonadotropic hypogonadism (congenital or acquired)-gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.
Routes: IM, patch, nasal gel, orally, topical cream
Should be given to men with consistent symptoms/signs of hypogonadism & low plasma testosterone levels (<3ng/ml). Safety and efficacy of Testosterone in men with “age-related hypogonadism” (also referred to as “late-onset hypogonadism”) have not been established!
SE: acne, gynecomastia, irritation at site of administration, headache, transfer to female partner; cholestatic jaundice syndrome, liver carcinoma, BPH, prostate cancer, DVT. [Women: clitoral hypertrophy, hirsutism, acne, amenorrhea]
- Liver cell tumors
- Peliosis hepatitis
Pregnancy category X; C-III
Spironolactone
Aldosterone antagonist
Regular
Lispro
Glargine
Which is fast acting?
Classic anabolic hormone: promotes carbohydrate metabolism; facilitates glucose, amino acid, triglyceride uptake & storage in liver, cardiac & skeletal muscle, adipose tissue
Insulin, regular, Actrapid/Humulin R/Novolin R—fast acting
Insulin, lispro, HumaLOG—very fast acting
Insulin, glargine, Lantus/Basaglar—basal level of insulin
Structurally similar to endogenous insulin; zinc ions provide stability; recombinant DNA technology
For use in insulin dependent diabetes mellitus
SE: injection site reaction, lipodystrophy; hypoglycemia
Nutrient considerations: alpha lipoic acid, vitamins C & E, n-acetyl cysteine protect insulin under oxidative stress; chromium improves insulin sensitivity (numerous ways); magnesium improves insulin sensitivity
Pregnancy category B
Glucagon
For rescue of hypoglycemia
Recombinant DNA technology; IV, IM, or SQ administration
CI in pheochromocytoma
Desmopressin
Modified arginine vasopressin: Desmopressin, DDAVP
Synthetic analogue of the natural pituitary hormone 8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation
Limits amount of water eliminated in urine
Used for diabetes insipidus, coagulation disorders (hemophilia A, von Willebrand’s disease type I)
SE: headaches, facial flushing, nausea, seizures, hyponatremia
Available po, sl, nasal spray, IV
Pregnancy category B
Oxytocin
Oxytocin, Pitocin/Syntocinon
The “love” hormone produced by posterior pituitary gland
Released during/after childbirth, with breastfeeding, at orgasm—creates bonding, evokes feelings of contentment, decreases anxiety; protects against stress
Used for medical (rather than elective) induction of labor, to control postpartum bleeding or hemorrhage
Available IV, nasal spray
Pregnancy category X
Bromocriptine,
Ergot alkaloid: Prolactin blocker
Dopamine receptor agonist
Uses: hyper-prolactinemia associated dysfunctions (amenorrhea with or without galactorrhea, infertility or hypogonadism); prolactin-secreting adenomas; acromegaly; Parkinson’s disease
SE: hypotension
Pregnancy category B
Somatropin
Growth hormone
Recombinant DNA growth hormone; assists growth of linear bone, skeletal muscle, and organs by stimulating chondrocyte proliferation and differentiation, lipolysis, protein synthesis, and hepatic glucose output; stimulates erythropoietin which increases red blood cell mass; exerts both insulin-like and diabetogenic effects; enhances the transmucosal transport of water, electrolytes, and nutrients across the gut
Labeled indications: growth failure in pediatrics; growth hormone deficiency in adults; cachexia of HIV; short bowel syndrome in patients receiving specialized nutritional support (Zorbtive).
SE: upper respiratory tract infection, arthralgia, arthropathy, headache, hypoesthesia, increased serum glucose, limb pain, myalgia, paresthesia, and peripheral edema; fatigue, fluid retention, gynecomastia, hyperglycemia, insomnia, joint stiffness, joint swelling, nausea, and anasarca (extreme generalized edema)
Pregnancy category C
Metformin
reduction %?
Uses: adjunct to diet and exercise to improve glycemic control in adultsand children with type 2 diabetes mellitus
Decreases glucose production in the liver, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization
Activates energy-regulating enzyme AMPK, which inhibits gluconeogenesis, fatty acid synthesis, and cholesterol synthesis
Increases insulin signaling
Reduction in HbA1C: 1.5-2%
Common side effects: lactic acidosis, diarrhea, nausea, nausea and vomiting, flatulence, asthenia
Uncommon but serious: Lactic acidosis
Nutrient depletions: vitamin B-12, folate
Contraindicated in patients with renal disease/dysfunction; patients with acute or chronic metabolic acidosis
Pregnancy category B
Metformin Considerations
Chromium enhances insulin activity and glucose control
Magnesium co-administered with sulfonylureas and/or metformin may improve insulin sensitivity and secretion—less drug warranted (850mg MgOH)
Vitamin E (natural, mixed tocopherols/tocotrienols) may enhance glycemic control
Glyburide
Reduction %
Sulfonylurea - Stimulate insulin release from pancreatic β-cells to overcome insulin resistance
Orally available; metabolized by liver
Adverse reactions: hypoglycemia, weight gain
Generally considered effective, reasonably safe, inexpensive
Typical reduction in HbA1C: 1-2%
Adverse reactions:
- hypoglycemia
- weight gain
- GI upset
Contraindicated in diabetic ketoacidosis
Nutrient Depletions, Sulfonylureas
CoQ10
Magnesium (diabetics tend to be deficient before drug therapy)
Pioglitazone
Thiazolidinedione - insulin sensitizer
Typical reduction in HbA1C: 1.5-2%
SE: heart failure & bladder cancer
BLACK BOX WARNING: may cause or worsen heart failure
Not to be used in DMI/with exogenous insulin or in patients with class III or class IV heart failure Caution in patients with edema Drug interactions: CYP2C8 Inhibitors and Inducers; no known nutrient wasting
Pregnancy category C
Liraglutide
GLP-1 agonist - Increases glucose-dependent insulin secretion
INJECTION
Typical reduction in HbA1c: 1%
Canaglifozin
SGLT-2 antagonist - reduces reabsorption of filtered glucose from the tubular lumen and lowers the renal threshold for glucose. Improvement of macrovascular vessels
Use in DMII with diet and exercise
SE: SUPER URINARY FREQUENCY (pollakiuria), necrotizing fasciitis, loss of genitalia, limb amputation
Pregnancy category C
**DIURETIC ON STEROID!! THIS SHIT IS DANGEROUS
Stigliptin
DPP-4 inhibitor - Prolongs active incretin levels for glucose regulation
SE: Anxiety, blurred vision, chills, cold sweats, confusion, cool, pale skin, depression, dizziness, fast heartbeat, headache, increased hunger, loss of consciousness, nausea, nightmares, seizures, shakiness, slurred speech, unusual tiredness or weakness
Pregnancy category B
1% reduction
They do not perform as well
Another injectable
Liothyronine, Levothyroxine, Lugol’s solution
Liothyronine, Cytomel (T3)
Levothyroxine, Synthroid/Levoxyl (T4)
Thyroid USP, (Armour) is a blend of T3 & T4 from dessicated pig thyroid
Lugol’s solution (LOW dose), elemental iodine and potassium iodide
Used in hypothyroidism & TSH pituitary suppression
Side effects are typically signs/symptoms of hyperthyroidism
Contraindicated in patients with untreated subclinical (suppressed serum TSH level with normal T3 and T4 levels) or overt thyrotoxicosis of any etiology and in patients with acute myocardial infarction. Levothyroxine is contraindicated in patients with uncorrected adrenal insufficiency.
Pregnancy category A
Hormones T4 and T4 work better with which nutrients?
No known depletions, but the hormones (T3, T4) work better with associated nutrients:
Selenium Zinc Iodine Copper Tyrosine (Adrenal support)
Propylthiouracil, Methimazole, Lugol’s solution
Lugol’s solution (HIGH dose)
Methimazole - Inhibits synthesis of thyroid hormone
Propylthiouracil (PTU) - Preferred agent in thyroid storm
Inhibits thyroid peroxidase, Inhibits conversion of T4 to T3 in the periphery
Labeled uses: hyperthyroidism (Grave’s disease or toxic multinodular goiter) for whom surgery or radioactive iodine therapy is not an appropriate treatment option; symptom control in preparation for thyroidectomy or radioactive iodine therapy
SE: rash, arthralgia;
life-threatening hepatotoxicity,
agranulocytosis, vasculitis, hypoprothrombinemia
Pregnancy category D
(Generally, methimazole is considered the safer of the two; not in pregnancy.)
If the pregnant woman is in thyroid storm, which hyperthyroid agent should you use? If not pregnant, which one is safer?
pregnant = PTU
Not pregnant = Methimazole
Melatonin
Hormone produced by pineal gland
Release is inhibited by light; promoted by dark
Useful for circadian rhythm entrainment; powerful free-radical scavenger & antioxidant—cancer, CVD, autoimmune diseases, depression, SAD
Useful in learning and memory—ADD/ADHD, ASD, Alzheimer’s
Over-the-counter status in the US; prescription elsewhere
Pregnancy category not assigned
hCG
Human chorionic gonadotropin (hCG)
Used to cause ovulation and treat infertility in women, increase sperm count in men, assist in testicular dropping into scrotum in young boys
SE: ovarian hyper-stimulation syndrome
Pregnancy category X
