EXAM #5: REVIEW Flashcards
List the vehicles that should be used on the scalp and hairy areas.
Lotion Solution Gel Aerosol Foam
List the vehicles that should be used on interriginous areas.
Lotion
Solution
Cream
List the vehicles that are good for drying.
Powder
Paste
Tincture
Aerosol
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?
Anaerobic
How is benzoyl peroxide commonly administered?
In combination with Erythromycin or Clindamycin
List the indications for the retinoid drugs.
1) Acne
2) Psoriasis
3) Skin aging
4) Skin cancer
List two side effects associated with the retinoid drugs.
1) TERATOGEN
2) Photosensitivity and increased risk of sunburn
What is the MOA of Tretinoin?
1) Reduces cohesiveness of comodomes
2) Codomolytic
3) Reduces keratinization
What is the MOA of Adapalene?
1) Reduced cellular proliferation
2) Reduced inflammation
3) Comedolysis
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?
Psoriasis
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
2) Acne
3) Enhanced fungal infection
4) Delayed wound healing
5) Hypopigmentation
List the Psoralen drugs. What is the MOA of these drugs?
Methoxsalen
Trioxsalen
Administered topically or orally; activated by light; intercalate with DNA
List four indications for the Psoralen drugs.
1) Alopecia
2) Cutaneous T-cell Lymphoma
3) Eczema
4) Psoriasis
List the long-term adverse effects of the Psoralens.
1) Photoaging
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
2) Wakefullness
3) Appetite/Satiety
List five clinical indications for a first generation antihistamine.
1) Allergic rhinitis
2) Allergic conjunctivitis
3) Urticaria
4) Motion sickness
5) Anti-emetic
What is the MOA of the H1 antihistamines?
“INVERSE AGONIST”
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.
Diphenhydramine
Promethazine
Hydroxyzine
Meclazine
List the three H1 antihistamines with the strongest sedative effects.
Diphenhydramine
Promethazine
Hydroxyzine
What H1 antihistamines have the strongest anticholinergic effects?
Diphenhydramine
Promethazine
What H1 antihistamines is the strongest alpha-1 antagonist?
Promethazine
List second generation antihistamines.
Foxofenadine Loratadine Desoloratadine Citrizine Levocitrazine Azelastine
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
2) Asthma
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?
Mineralcorticoid
Glucocorticoid
List the major adverse effects seen with elevated cortisol.
1) Salt/water retention
2) Hypokalemia
3) HTN
What is Primary Adrenal Insufficiency? What are the symptoms?
Autoimmune or tuberculoid destruction of the adrenal cortex leading to:
- Hypotension
- Hyponatremia
- Hypokalemia
- Hypoglycemia
How do you treat Primary Adrenal Insufficiency?
1) Cortisol
2) Increase Na+ intake
3) Fludrocortisone
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?
Ketoconazole
Metyrapone
Mifepristone
What is the MOA of Ketoconazole to treat Cushing’s?
Antifungal that inhibits 17-a hydroxylase
What toxicity is associated with Ketoconazole?
Liver toxicity
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?
Growth retardation
What are the local adverse effects of inhaled glucocorticoids to treat asthma?
1) Dysphonia
2) Oropharyngeal candidiasis
3) Cough
List four functions of the thyroid hormones.
1) Growth
2) Development
3) Body temperature
4) Energy metabolism
What enzyme converts T4 into T3?
5’-deiodinase
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.
Levothyroxine (T4)
Liothyronine (T3)
Liotrix (Both)
List the adverse effects of thyroid replacement in children,
Restlessness
Insomnia
Accelerated bone maturation
List the adverse effects of thyroid replacement in adults.
Nervousness Heat intolerance Palpitations Tachycardia Weight loss
List the adverse effects of thyroid replacement in the elderly.
A-fib
Osteoporosis
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.
Methimazole
Propylthioruacil (PTU)
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.
Potassium iodide
Lugol’s Solution
What are the clinical indications for the iodides?
1) Thyroid storm
2) Preoperative prep for surgery
What adverse effect is associated with the iodides?
Cold sx.
List the anion inhibitors that block the NIS transporter.
Percholrate
Pertechnetate
Thiocyanate
What is the clinical indication for the anion inhibitors?
Iodide induced hyperthyroidism
List four antithyroid adjuncts.
1) Propanolol
2) Diltiazem
3) Barbiturates
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.
Methyltestosterone (17-alkylated)
Testosterone enanthate (ester)
Testosterone
List the adverse effects of androgen therapy.
1) Reduction in spermatogenesis/testis size
2) Acne
3) Polycythemia
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
2) BPH
3) Prostate cancer
4) Alopecia
List the androgen receptor antagonists.
Flutamide
Biclatumide
What adverse effects are associated with the androgen receptor antagonists?
Gynecomastia
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.
Leuprolide
Goserelin
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?
Degarelix
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?
Finasteride
Dutasteride
What are the clinical indications for the 5-a reductase inhibitors?
BPH
Alopecia
What are the key adverse effects associated with the 5-a reductase inhibitors?
Impotence
Gynecomastia
Low PSA–>false negative
List the PDE-5 inhibitors.
Sidenafil
Vardenafil
Tadalafil
What drugs are contraindicated with PDE-5 inhibitors?
HIV protease inhibitors
Nitrates
What adverse effects are associated with PDE-5 inhibitors?
1) Priapism
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?
Decreased contraction
What is the MOA of progesterone to decrease uterine contraction?
1) Decreased prostaglandin production
2) Maintenance of relaxin
What is the primary synthetic estrogen?
Ethinyl estradiol
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.
1) Hypogonadism
2) Hormone replacement therapy
3) Contraception
4) Acne
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?
CAD
CVA
PE
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?
Endometrial
List the progesterones.
Medroxyprogesterone (MPA)
Norethindrone
Norgestrel
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
2) Nausea
3) Mastalgia
4) Edema
5) Headache
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
4) Acne
5) Hirsutism
6) Vaginal infection
7) Amenorrhea
List the “severe” adverse effects of birth control.
1) Thromboembolic disease
2) MI
3) CVA
4) GI disorders e.g cholestasis
5) Depression
6) Cancer
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
2) Anticonvulsants
3) HIV antiretrovirals
What is the clinical indication for Clomiphene?
Fertility drug
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
2) Endometriosis
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
4) Acne
5) Hirsutism
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
3) Lethargy
List the anti-progesterone drugs.
Mifepristone
Ulipristal
*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.
1) Glucose
2) Amino acids
3) Incretins
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.
Insulin lispro
Insulin aspart
Insulin glulisine
What is an intermediate acting insulin?
NPH
Forms protamine insulin complexes
What are the two long-acting insulins?
Glargine
Detemir
What is the MOA of metformin?
1) Decreased hepatic glucose output
2) Increased peripheral glucose utilization
List the Sulfonylureas.
Glimepiride
Glipizide
Glyburide
List the meglitinides.
Repaglinide
Nateglinide
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?
Weight gain
Hypoglycemia
List the glucosidase inhibitors.
Acrabose
Miglitol
List the Thiazolindinediones.
Pioglitazone
Rosiglitazone
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?
1) Anorexia
2) Hypoglycemia
3) Delayed drug absorption
List the incretin mimics.
Exenatide
Liraglutide
List the DPP inhibitors.
Sitagliptin
Saxagliptin
Linagliptin
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?
Convulsions
Coma
Cardiac conduction
What is the mnemonic to remember the aspirin OD Toxidrome?
DAFT HID
Deafness Appear flushed Fever Tinnitus Hyperventilation Increased sweating Dizziness
What is a copy number variation?
Duplication or deletion of an entire gene
What drugs will have altered metabolism because of CYP2D6 polymorphisms?
Tamoxifen
Codiene
Paroxetine
What drugs will have altered metabolism because of CYP2C19 polymorphisms?
Clopidogrel
Omperazole
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?
DDP
What gene codes for thymidylate synthetase?
TYMS
Do polymorphisms in TYMS result in pharmcokinetic or pharmacodynamic changes?
Pharmacodynamic
What inactivates 6-MP?
TPMT
What do ERa genes code for? What drugs will be effected by ERa polymorphisms?
Estrogen receptors
- Estrogen
- Progesterone
What have ERa polymorphisms been associated with in estrogen HRT?
Increased HDL