Test 5 Flashcards
What four antibiotics are used to treat acne?
Clindamycin and erythromycin
Metronidazole and sodium sulfacetamide
What are the two MOAs of Azelaic Acid?
reduces keratinization
keratolysis
What is the MOA of salicyclic acid?
breaks hydrogen bonds in stratum corneum
What is the MOA of tretinoin? What is tretinoin inactivated by?
induces mitosis that extrudes acne
benzoyl peroxide
What is the difference between adapalene and tretinoin?
adapalene can be complexed with benzoyl peroxide
What is the MOA of accutane?
induces apoptosis of sebum producing glands
What is the MOA of tazarotene?
reduces inflammation
What is Acitretin used to treat? What increases acitretins half-life?
psoriasis
alcohol
What is the MOA of Calcipotriene? Used to treat?
inhibits proliferation of keratinocytes
Psoriasis
Is hydrocortisone weak, intermediate or strong?
weak
Is Mometasone furoate weak, intermediate or strong?
intermediate
Is Clobetasol proprionate weak, intermediate or strong?
strong
What are the two UV active compounds?
Methoxsalen and Trioxsalen
What drug functions like cromolyn?
Nedocromil
What are H1 Antagonists?
Inverse agonists
Which anti-histamine can act as a local anesthetic?
Promethezine
Which anti-histamine has anti-serotonin properties?
Cyproheptadine
Which four antihistamines are used for motion sickness?
Diphenhydrimine/hydroxyzine/Promethazine/Meclizine
Which three antihistamines are known for their Highest sedation?
Diphenhydramine/promethazine/hydroxyzine
Which two antihistamines are known for their anticholinergic activity?
Diphenhydramine/promethazine
Which antihistamine is known for its anti-alpha-adrenergic?
Promethazine
Antihistamines can interfere with what other group of drugs? Specifically, what effects?
MAOIs
anti-muscarinic effects
Which tricyclic can block histamine receptors? Which isotypes?
Doxepin
H1 and H2
What type of antagonist is ketotifen? What other cell type can it stabilize?
H1
stabilize basophil and mast cells
What is the function of 11βHSD2? What type of tissues is this enzyme found?
convert cortisol into inactive cortisone
mineralocorticoid
What is the function of 11βHSD1?
convert cortisone into cortisol
What enzyme does Wauson say ketoconazole can inhibit?
17α-hydroxylase
11β-hydroxylase
What drug does Wauson say can inhibit 11β-Hydroxylase?
Metyrapone
What are the four inhaled glucocorticoids?
Budesonide
Fluticasone
Mometasone
Triamcinolone
What is the relationship between inhaled glucocorticoids and β2 adrenergic receptors?
increase the synthesis of each other
Which glucocorticoid has low protein binding?
dexamethasone
What are the three thyroid drugs?
Levothyroxine/Liothyronine/Liotrix
What is levothyroxine composed of?
T4
What is Liothyronine composed of?
T3
What is Liotrix composed of?
T3/T4 mix
What are the two anti-thyroid agents? MOA?
Methimazole and Propylthiouracil
inhibit TPO
Which anti-thyroid is preferred during pregnancy? Why?
Propylthiouracil
more protein bound
What are the three anion thyroid inhibitors? MOA?
Perchlorate/Pertechtenate/Thiocyanate
inhibit uptake of iodide
Why can propranalol be used to treat hyperthyroidism?
inhibit the conversion of T4 into T3
What cell synthesizes tesosterone in men?
Leydig
What enzyme is expressed in Leydig cells? What rxn does this enzyme catalyze?
17-βHSD
converts androstenedione into testosterone
Is testosterone bound to albumin bioavailable or not bioavailable?
bioavailable
Is testosterone bound to SHBG bioavailable or not bioavailable?
not bioavailable
What does Testosterone do to blood glucose levels?
Lowers
What does Testosterone do to bone?
enhances formation
What does estradiol do to epiphysial plates?
close them
What is defective during Primary Hypogonadism?
testicular defect
Is primary or secondary Hypogonadism hypergonadotropic?
primary
Where is the defect in Secondary Hypogonadism?
hypothalamus/pituitary
Where are testosterone esters used?
replacement in hypogonadal men
What are Alkylated Testosterones used for?
anabolic steroids
Do testosterone esters or or alkylated testosterone carry a higher risk for hepatic cancers?
Alkylated
What is the MOA of flutamide and bicalutimide?
androgen receptor antagonists
In what two situations are flutamide and bicalutimide used?
prostate cancer
testosterone surge due to GnRH agonists
What is the main MOA of enzalutimide?
androgen receptor antagonist
What are the three additional MOAs of enzalutamide?
decrease txn
decrease DNA binding
blocks coactivator
What are the two GnRH agonsits?
Leoproldie and Goserelin
What drug should be co-administered with a GnRH analogue? Why?
androgen receptor antagonist
prevent testosterone surge
What is the GnRH antagonist?
Degarelix
What drug blocks 17α-Hydroxylase? What is the main side-effect? Used to treat?
Abiraterone
HTN
Metastatic prostate cancer
What class of drugs are used to treat alopecia?
5α-Reductase Inhibitors
What are two side effects of 5α-Reductase Inhibitors?
Gynocomastia and Impotence
What two patients dont respond well to Sildenafil?
nerve damage (diabetes)
Radical prostatectomy
What is the function of the ethinyl group?
increases half-life
What does estrogen do to the blood?
increase plasma proteins
decrease anti-thrombin
Why do estrogens cause bloating?
loss of intravascular fluid
What is the function of medroxyprogesterone?
long acting contraceptive
Why does progesterone cause a decrease in uterine contractions?
progesterone causes a decrease in prostaglandin synthesis
Which molecule is responsible for glucose intolerance during pregnancy?
progesterone
What has a poor effect on lipids, estrogens or progesterones?
progesterones
What is the MOA of clomiphene?
estrogen receptor partial agonist
What are two adverse effects of clomiphene?
multiple births
hot flashes
Where is tamoxifen an agonist?
bone
Where is tamoxifen a partial agonist?
endometrium
Where is tamoxifen an antagonist?
uterus and HPG
Where is raloxifen an agonist?
bone
Where is raloxifene an antagonist?
uterus
breast
HPG
Why can Danazol cause hirsutism?
metabolite is an androgen
What are the two uses of danazol?
fibrocystic change
endometriosis
What are the two aromatase inhibitors?
Anastrozole
letrozole
What is the MOA of mifepristone? Timeframe?
progesterone antagonist
less than 7 weeks
What is the MOA of Ulipristal? Timeframe?
progesterone partial agonist
less than 5 days
What effect do the anti-progesterones have on uterine contractions? Why?
decrease uterine contractions
decrease prostaglandin production
What GLUT transporter does insulin up-regulate?
GLUT 4
What is the MOA of metformin? Via what protein?
inhibit hepatic output of glucose
AMPK activation
What is the main side effect of metformin?
diarrhea
What are the three sulfonylureas?
Glipizide
glyburide
Glimepiride
What is the MOA of the sulonylureas?
inhibition of ATP sensitive K+ channel resulting in insulin release
What are the two Meglitinides?
Repaglinide
Nateglinide
What is the MOA of Repaglinide and Nateglinide?
same as sulfonylureas
What are the two disaccharidase inhibitors? What enzyme do they inhibit?
Acarbose and Miglitol
Glucosidase
What are the two Thiazolidinediones?
Pioglitazone
Rosiglitazone
What is the MOA of Pioglitazone and Rosiglitazone? Via what protein?
increase expression of GLUT4
activation of PPAR
What is the MOA of pramlintide?
inhibit glucagon release
What are the two incretins? MOA?
Exanetide and Liraglutide
promote secretion of insulin
What is the MOA for all Dipeptidyl Peptidase inhibitors?
inhibit incretin degradation
What is the common suffix for all Dipeptidyl Peptidase inhibitors?
-Gliptin
What is the MOA of the -gliptins?
Inhibit incretin degradation
What property of ADME is least effected by aging?
absorption
Is phase I or Phase II metabolism more effected in elderly? Increase or decrease?
Phase I
decrease
Does anything happen to the maintenance dose of Phase II drugs?
no
Does anything happen to the maintenance dose of Phase I drugs?
decrease
What is the purpose for the Cockroft-Gault equation?
account for the decreasing muscle mass in elderly
Are elderly more sensitive or less sensitive to opioids?
more sensitive
What is the MOA of isotretinoin?
induces apoptosis of sebum producing cells
What is the IgE receptor?
Fc-Gamma-R1
Which histamine receptor mediates itch?
H1
Which histamine receptor mediates bronchoconstriction?
H1
Which histamine receptor is found in the heart?
H2
Which selectin does histamine up-regulate?
P-selectin
What type of drug is Chlorpheniramine?
H1 antagonist
What type of drug is pyrilamine?
H1 antagonist
Which anti-histamine can act as a local anesthetic?
Promethazine
Which anti-histamine can block the D2 receptor?
Promethazine
Where is the defect during Primary Adrenal Insufficiency?
adrenal
Where is the defect during Secondary Adrenal Insufficiency?
decreased ACTH
Does dexamethasone bind the MR?
no
What does high [Iodide] do to thryoid hormone synthesis?
high = inhibits
What does low [Iodide] do to thryoid hormone synthesis?
low = activates
What does thyroid hormone do to β-adrenergic receptor levels?
increase
What does thyroid hormone do to α-adrenergic receptor levels?
decrease
Which is preferred for thyroid storm, methimazole or propylthiouracil?
propylthiouracil
What are the two causes of Hypergonadotropic Hypogonadism?
Klinefelters and Cryptorchidism
What are the two 5α Reductase Inhibitors?
Finasteride and Dutasteride
Does estrogen or progesterone cause hirsutism?
progesteorne
Does estrogen or progesterone cause acne?
progesterone
Does estrogen or progesterone cause poor lipid metabolism?
progesterone
What is the use of clomiphene?
fertility drug
What two tissues express GLUT4?
muscle and adipocytes
What is the legal definition of a poison?
LD50 less than 50 mg/Kg
What are the two emetics?
Apomorphine and Ipecac
What two drugs are administered to treat acetylcholine OD?
2-PAM and atropine
What three drugs are administered to treat cyanide poisoning?
sodium nitrite
amyl nitrite
sodium thiosulfate
What is the Tx for botulinum toxin?
ABC antibodies
What is the difference betwen naloxone and naltrexone?
naltrexone is longer lasting
Exposure of hemoglobin to what two substances can result in methemoglobinemia?
nitrites and sulfa drugs
What is the Tx for methemoglobinemia?
methylene blue
Which opiate can cause convulsions? What is the active metabolite responsible for this?
Demerol
Meperidine
Which layer of the epidermis can act as a reservoir?
stratum corneum
What is the rationale to use barbiturates to treat hyperthyroidism?
increase metabolism of T4
What is the rationale to use Bile Acid Sequestrans to treat hyperthyroidism?
increase biliary secretion of T4
Long term use of what anti-diabetic drug can deplete B12?
Metformin
What is the MOA of Benzoyl Peroxide?
releases O2 that kills anaerobes
What are the three MOAs of all retinoids?
decrease cohesiveness of epithelial cells
induces mitotic activity
reduces keratinization
What two interleukin molecules does Calcipotriene inhibit?
IL2 and IL6
What type of drug is fludricortisone?
mineralocorticoid
What does Mifepristone act like at a high dose?
glucocorticoid antagonist
What can a large dose of glucocorticoids stimulate the synthesis of?
gastric acid
What can too much thyroid hormone do to the bones in the elderly?
osteoporosis
What organ can be adversely effected by propylthiouracil?
hepatitis
What is the side-effect of perchlorate?
aplastic anemia
What drug is used in combination with Abiraterone?
Prednisone
Other than erections, what can sildenafil be used for?
pulmonary HTN
Would estrogen increase or decrease available testosterone? Why?
decrease
increase hepatic SHBG levels
What is the function of incretins?
promote insulin secretion
What is the function of the Dipeptidyl Peptidase Inhibitors?
breakdown incretins
What does capacity limited mean?
clearance is a reflection of liver enzyme function
What does Flow Limited mean?
only dependent on amount of blood reaching liver
Would the elderly have an increased or decreased response to β-blockers?
decreased
According to Wauson, which two drugs have the highest anti-cholinergic activity in the elderly?
Tricyclics and Paroxetine
What is a synonymous SNP?
amino acid is not changed
What is a nonsynonymous SNP?
amino acid is changed
What is CNV?
deletion or duplication of a gene
What is a population polymorphism?
polymorphism that changes across races
What is a cosmopolitan polymorphism?
polymorphism that changes across populations
What three drugs are metabolized by CYP2D6?
codeine
paroxetine
tamoxifen
Does 2D6 inactivate or activate tamoxifen?
Activate
Does 2D6 inactivate or activate CODEINE?
activate
Does 2D6 inactivate or activate paroxetine?
inactivate
What three drugs are acted on by 2C19?
Clopidogrel
omeprazole/Lansoprazole
Does 2C19 activate or inactivate Clopidogrel?
activate
Does 2C19 activate or inactivate Omeprazole?
inactivate
What Cytp450 acts on warfarin? Activate or Inactivate?
2C9
inactivate
What two drugs does act on EGFR?
Erlotinib and Cetuximab
Is 5FU activated or inactivated by DPD?
inactivated
What does TMPT do to 6MP?
inactivate
What protein clears simvistatin?
SLC01B1
What did the ER mutation do during HRT? Kinetics or dynamics?
increased HDL increase
dynamics
What do ADRB2 mutations produce? Kinetics or dynamics?
lesser affinity for albuterol
dynamics
Which IL molecule has a poor response to IFN-α?
IL28
Do mutations in TS effect the pharmacodynamics or pharmacokinetics of 5FU?
dynamics
Which topical agent can inhibit neutrophils?
benzoyl peroxide
Which topical agent can inhibit lymphocytes?
Calcipotriene
What are the two drawbacks to using iodide to suppress thyroid function?
only 2-8 weeks suppression
rebound thyrotoxicosis
What are the two MOAs of iodide inhibiting thyroid function?
inhibit proteolysis of TGB
inhibit organification
Which emergency contraceptive is more effective, combined or progestin only?
progestin only
What are the three 1st generations sulfonylureas?
Tolbutamide
Chlorpropramide
Tolazamide
What population cant receive Glucosidase Inhibitors?
people with GI diseases
What is the adverse effect of the -litazones?
cardiovascular
What is the toxicity of Exenatide and Liraglutide?
acute pancreatitis
