Flashcards in EXAM #5: REVIEW Deck (156):
List the vehicles that should be used on the scalp and hairy areas.
List the vehicles that should be used on interriginous areas.
List the vehicles that are good for drying.
What bacteria can be treated with Azelaic acid?
P. acnes and S. epidermidis
Describe the MOA of Azelaic acid.
1) Reduces inflammation
2) Reduces keratinization
3) Keratolytic and induces desquamation
What side effects are associated with Azeliac acid?
1) Lightening of the skin
2) Skin dryness
What is the MOA of benzoyl peroxide?
Release ROS that are harmful to anaerobic bacterial species
What type of bacteria is benzoyl peroxide effective against?
How is benzoyl peroxide commonly administered?
In combination with Erythromycin or Clindamycin
List the indications for the retinoid drugs.
3) Skin aging
4) Skin cancer
List two side effects associated with the retinoid drugs.
2) Photosensitivity and increased risk of sunburn
What is the MOA of Tretinoin?
1) Reduces cohesiveness of comodomes
3) Reduces keratinization
What is the MOA of Adapalene?
1) Reduced cellular proliferation
2) Reduced inflammation
What is the MOA of Isotretinoin?
Induces apoptosis of sebum producing cells in sebaceous glands
What is the MOA of Tazarotene?
1) Decreases inflammation
2) Reduces epidermal inflammation
What are the clinical indications for Tazarotene?
Acne and Psoriasis
What is the clinical indication for Acritretin?
Severe, reluctant psoriasis
What is the clinical indication for Calcipotriene?
What is the MOA of Calcipotriene?
- Binds Vitamin D receptor
- Gene transcription changes are beneficial in PSORIASIS
List five adverse effects of topical corticosteroids.
1) Epidermal atrophy
3) Enhanced fungal infection
4) Delayed wound healing
List the Psoralen drugs. What is the MOA of these drugs?
Administered topically or orally; activated by light; intercalate with DNA
List four indications for the Psoralen drugs.
2) Cutaneous T-cell Lymphoma
List the long-term adverse effects of the Psoralens.
2) Actinic keratoses
3) Nonmelanoma skin cancer
List the three primary locations of H2 receptors.
1) GI parietal cells
2) Cardiac muscle
3) CNS neurons
What are the three general functions of histamine in the CNS?
1) Release of pituitary hormones
List five clinical indications for a first generation antihistamine.
1) Allergic rhinitis
2) Allergic conjunctivitis
4) Motion sickness
What is the MOA of the H1 antihistamines?
List five major side effects of the first generation antihistamines and the receptor association with that effect.
- CNS depression (H1)
- Dry mouth and urinary retention (M -- anticholinergic)
- Increased appetite and weight gain (5-HT)
- Dizziness and postural hypotension (Alpha-1)
List the four H1 antihistamines with the strongest anti-emetic effects.
List the three H1 antihistamines with the strongest sedative effects.
What H1 antihistamines have the strongest anticholinergic effects?
What H1 antihistamines is the strongest alpha-1 antagonist?
List second generation antihistamines.
What are the clinical pearls the remember with Foxfenadine administration?
1) Decrease dose with renal dysfunction
2) Don't combine with antacids
What is the MOA of Cromolyn and Nedocromil?
Stabilization of mast cells to prevent degranulation
What are the three clinical indications for Cromolyn and Nedocromil?
1) Allergic rhinitis
2) Allergic conjunctivitis
3) Exercise induced asthma
List two indications for Omalizumab.
1) Chronic urticaria
What is Doxepin?
TCA used to treat chronic urticaria
What is Ketotifen?
H1 antihistamine with additional mast cell stabilizing characteristics
*Used in an ophthalmic preparation for allergic conjunctivitis*
What two receptors can cortisol bind to and activate?
List the major adverse effects seen with elevated cortisol.
1) Salt/water retention
What is Primary Adrenal Insufficiency? What are the symptoms?
Autoimmune or tuberculoid destruction of the adrenal cortex leading to:
How do you treat Primary Adrenal Insufficiency?
2) Increase Na+ intake
Aside from iatrogenic Cushing's Disease, what are the alternate etiologies of Cushing's?
1) Pituitary tumor with increased ACTH
2) Ectopic ACTH tumor
3) Adrenal tumor
What are the three drug therapies for Cushing's Syndrome?
What is the MOA of Ketoconazole to treat Cushing's?
Antifungal that inhibits 17-a hydroxylase
What toxicity is associated with Ketoconazole?
What is the MOA of Metyrapone to treat Cushing's?
Inhibits 11-B hydroxylase
*Note that this is also used in the diagnosis of ACTH production*
What is the MOA of Mifepristone?
Glucocorticoid receptor antagonist
What are the specific indications for Mifepristone?
1) Inoperable ectopic ACTH production
2) Adrenal carcinoma
What is the MOA of inhaled glucocorticoids in the treatment of asthma?
- Reduced proliferation and hypertrophy of airway smooth muscle
- Prevents leakage of vascular endothelium
- Reduces adhesion of molecules to vascular epithelium
- Increased epithelial integrity
What is a significant adverse effect of inhaled glucocorticoids, especially in kids?
What are the local adverse effects of inhaled glucocorticoids to treat asthma?
2) Oropharyngeal candidiasis
List four functions of the thyroid hormones.
3) Body temperature
4) Energy metabolism
What enzyme converts T4 into T3?
What is the effect of low thyroid hormone levels on the SNS?
1) Increased Beta-adrenergic receptors
2) Decreased Alpha-adrenergic receptors
List the causes of primary hypothyroidism.
1) Congenital i.e. Cretinism
2) Autoimmune Thyroiditis
3) Iodide deficiency
4) Other i.e. surgery, radiation, and meds like Lithium
List the drugs used to treat hypothyroidism.
List the adverse effects of thyroid replacement in children,
Accelerated bone maturation
List the adverse effects of thyroid replacement in adults.
List the adverse effects of thyroid replacement in the elderly.
List five causes of primary hyperthyroidism.
1) Grave's Disease
2) Thyroid adenoma/ carcinoma
3) Autoimmune thyroiditis
4) Thyroid storm
5) Excess iodide
List the thioamides.
What is the MOA of the thioamides?
Inhibition of thyroid hormone synthesis in the thyroid follicle
What adverse effects are associated with the thioamides
PTU= severe hepatitis
Methimazole= altered taste and smell
List the iodides.
What are the clinical indications for the iodides?
1) Thyroid storm
2) Preoperative prep for surgery
What adverse effect is associated with the iodides?
List the anion inhibitors that block the NIS transporter.
What is the clinical indication for the anion inhibitors?
Iodide induced hyperthyroidism
List four antithyroid adjuncts.
4) Bile acid sequestrates
What is the utility of Diltiazem in the treatment of hyperthyroid?
Good alternative to propanolol in patients with asthma
What does FSH induce the synthesis of in the Sertoli cells?
Androgen Binding Protein
List the metabolic effects of the androgens.
1) Increased muscle growth
2) Liver production of serum proteins
3) Kidney synthesis of EPO
4) Bone growth and bone marrow stem cell production
List the three theraputic androgen preparations.
Testosterone enanthate (ester)
List the adverse effects of androgen therapy.
1) Reduction in spermatogenesis/testis size
4) Prostatic enlargement
5) Na+ and H20 retention leading to HTN
6) Increased LDL and decreased HDL leading to atherosclerosis
7) Mood swings, depression, and aggression
What are the indications of antiandrogen therapy in makes?
1) Percocious puberty
3) Prostate cancer
List the androgen receptor antagonists.
What adverse effects are associated with the androgen receptor antagonists?
Mild liver toxicity
What is the MOA of Enzalutamide?
Androgen receptor antagonist that also:
1) Inhibits nuclear translocation of the androgen receptor
2) Blocks DNA binding
3) Blocks transcriptional coactivator recruitment
List the GnRH agonists.
What are the outcomes of constantly elevated GnRH as seen with the GnRH agonsits?
1) Desenzitization of GnRH receptors on pituitary
2) Decreased LH production and secretion
3) Decreased Testosterone
What is the hallmark GnRH antagonist?
What is MOA of Abiraterone?
Androgen synthesis inhibitor that inhibits 17-alpha hydroxylase
*Indicated for metastatic prostate cancer*
What are the two 5-a reductase inhibitors?
What are the clinical indications for the 5-a reductase inhibitors?
What are the key adverse effects associated with the 5-a reductase inhibitors?
Low PSA-->false negative
List the PDE-5 inhibitors.
What drugs are contraindicated with PDE-5 inhibitors?
HIV protease inhibitors
What adverse effects are associated with PDE-5 inhibitors?
2) Sudden vision loss
3) Cardiac events
Outline the two-cell hypothesis of steroidogenesis in the ovary.
LH= increased androstenedione synthesis in Theca cells, which is converted into testosterone
FSH= Converts testosterone into estradiol in the granulosa cells
What effect does progesterone have on uterine contractions?
What is the MOA of progesterone to decrease uterine contraction?
1) Decreased prostaglandin production
2) Maintenance of relaxin
What is the primary synthetic estrogen?
What are conjugated equine estrogens? How are these used clinically?
Natural water-soluble estrogen sulfates
- Higher dose vs. synthetics
- Used for hormone replacement therapy
List four indications for estrogen replacement therapy.
2) Hormone replacement therapy
What are the three goals of estrogen used in hormone replacement therapy?
1) Maintain bone density
2) Suppress hot flashes
3) Suppress urogenital atrophy
What are four risks specifically associated with estrogen in hormone replacement therapy?
Invasive breast cancer
What is the MOA of estrogen as a treatment for acne?
1) Suppression of steroidogensis
2) Increased SHBG to decrease free testosterone
What are the adverse effects of non-HRT estrogen therapy?
1) Breast tenderness
2) Endometrial hyperplasia
3) Increased blood coagulation
What cancer risk is increased by combined HRT?
Invasive breast cancer
What cancer risk is increased with estrogen monotherapy?
List the progesterones.
What are the adverse effects associated with progestins?
1) Breakthrough bleeding
2) Impaired glucose tolerance
3) Changes in lipid metabolism: increased LDL and decreased HDL
List the "mild" adverse effects of birth control.
1) Estrogen-mediated breakthrough bleeding
6) Withdrawal bleed failure
7) Serum protein changes
List the "moderate" adverse effects of birth control.
1) Progestin mediated breakthrough bleeding
2) Weight gain
3) Increased skin pigmentation
6) Vaginal infection
List the "severe" adverse effects of birth control.
1) Thromboembolic disease
4) GI disorders e.g cholestasis
List the benefits of oral contraception, aside from contraception.
1) Reduced risk of ovarian and endometrial cancer
2) Reduction in dysmenorrhea/ endometriosis
3) Decreased incidence of ectopic pregnancy
4) Decreased benign breast disease
5) Increased Hb concentrations
6) Suppression of acne and hirsutism
List the contraindications to estrogen containing birth control.
1) Known or suspect breast cancer
2) Thromboembolic disorder
3) Liver disease
4) Cardiovascular disease
5) Smoker over 35 y/o
List three classes of drugs that will induce hormone metabolsim.
1) St. John's Wort
3) HIV antiretrovirals
What is the clinical indication for Clomiphene?
What is the MOA of Clomiphene?
Partial agonist that blocks negative feedback on LH and FSH
*Thus, it increases the likelihood of ovulation
What two adverse effects are associated with Clomiphene?
1) Hot flashes
2) Multiple births
What is the effect of SERMS on the endometrium?
Partial agonists that increase proliferation of the endometrium
What are the adverse effects associated with Tamoxifen?
1) Hot flashes
2) Endometrial cancer
3) Nausea and vomiting
*Note that vs. Raloxifene, which is hot flashes only*
What are the indications for Dananzol?
1) Fibrocystic breast disease
What is the MOA of Dananzol?
- Decreases estrogen concentrations in blood
- Displaces estrogen from serum proteins, which increases excretion
List the adverse effects assocaited with Dananzol.
1) Hot flashes
2) Weight gain
3) Oily skin
What is the MOA of anaztrozole and letrozole?
- Aromatase inhibitors
- Prevent the conversion of testosterone to estrogen
What adverse effects are associated with anaztrozole adn letrozole?
1) GI disturbances
2) Hot flashes
List the anti-progesterone drugs.
*Note that Mifepristone (progesterone antagonist) is followed by MISOPROSTOL--likely test question
What is the MOA of Ulipristal?
Partial progesterone agonist
List the factors that will increase insulin secretion.
2) Amino acids
4) Epinephrine/ B2 stimulation
5) Vagal stimulation
What is the major metabolic response to insulin (at the cellular level)?
Translocation of GLUT-4 transporters from the cytoplasmic compartment to the plasma membrane
List the rapid acting insulins.
What is an intermediate acting insulin?
*Forms protamine insulin complexes*
What are the two long-acting insulins?
What is the MOA of metformin?
1) Decreased hepatic glucose output
2) Increased peripheral glucose utilization
List the Sulfonylureas.
List the meglitinides.
What is the MOA of the sulfonylureas and the meglitinides?
Inhibition of the ATP-sensitive K+ channel in beta-cells
What adverse effects are associated with the sulfonylureas and meglitinides?
List the glucosidase inhibitors.
List the Thiazolindinediones.
What is the MOA of the Thiazolindinediones?
Increased expression of GLUT-4
What is the MOA of Pramlintide?
Synthetic amylin that
- Inhibit glucagon release
- Inhibits gastric emptying
- Has an anorexic effect
What adverse effects are associated with Pramlintide?
3) Delayed drug absorption
List the incretin mimics.
List the DPP inhibitors.
List four cardiovascular changes in the elderly that can result in altered pharmacokinetics.
1) Decreased sensitivity to B-adrenergic stimulation
2) Decreased baroreceptor activity
3) Decreased CO
4) Increased TPR
How is hepatic metabolism altered in the elderly?
1) Decreased hepatic blood flow
2) Reduced activity of phase I enzymes
What does ALD stand for?
Average Lethal Dose
What is the mnemonic to remember the anticholinergic toxidrome?
- Hot as a hare: increased body temperature
- Blind as a bat: mydriasis (dilated pupils)
- Dry as a bone: dry mouth, dry eyes, decreased sweat
- Red as a beet: flushed face
- Mad as a hatter: delirium
What are the three C's of TCA overdose?
What is the mnemonic to remember the aspirin OD Toxidrome?
What is a copy number variation?
Duplication or deletion of an entire gene
What drugs will have altered metabolism because of CYP2D6 polymorphisms?
What drugs will have altered metabolism because of CYP2C19 polymorphisms?
What is the role of CYP2C9 in Warfarin therapy?
CYP2C9 metabolizes warfarin
- Nonfucntional enzyme= increased warfarin concentration and adverse effects
What is the MOA of 5-dUMP?
Inhibition of thymidylate synthetase
What enzyme inactivates 5-FU?
What gene codes for thymidylate synthetase?
Do polymorphisms in TYMS result in pharmcokinetic or pharmacodynamic changes?
What inactivates 6-MP?
What do ERa genes code for? What drugs will be effected by ERa polymorphisms?