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232 Cards in this Set

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What antibiotic for Staph/Strep infection, especially clean surgical prophylaxis
Possibly used if UTI is suspected
1st Generation Cephalosporin
Cefazolin
What antibiotic for Staph/Strep infection,
Serious adult pneumonia (name the exception),
Serious pediatric pnemonia
2nd Gen. Cephalo.
Cefuroxime (only 2nd gen cephalo with decent CNS penetration)

Exception is Pseudomonas
Name antibiotic (2 cephalos) and 1 other antibio

Toxicity: antabuse-like reactions to alcohol
Cefotetan (2nd)

Cefoperazone (3rd)

Metranidazole
Name antibiotic (2)

Use: combination of anaerobes (Bacteroides) & community acquired aerobes; intra-abdominal/pelvic infections
Cefotetan
Cefoxitin

Both 2nd
Name antibiotic

Use: reserved for serious hospital acquired infections
Cefepime (4th)
What two cephalosporins would you give for meningitis?
Cefotaxime
Ceftriaxone

Both 3rd
What antibiotic would you give if someone has Pseudomonas?
3rd gen cephalo:

Ceftazidime
AG+Beta lactam
Cefepine
Fluro (esp. Cipro)
Carbepnem (except Ertapenem)
Never used for anaerobes & MRSA, Enterococci, Listeria
Cefepime

Cephalosporins are NOT used against MRSA, Enterococci, and Listeria
Use: skin & soft tissue infections, due to Staph/Strep (except MRSA)

Two antibiotics = ?
Cephalexin
Cefadroxil
5 drugs that are used as backup for resp. infections (H.flu, Moraxella) that produce β-lactamase; occasionally UTIs
Cefaclor
Cefuroxime axetril
Cefprozil
Cefpodime proxetil
Cefixime

Oral cephalosporins (2nd and 3rd)
Which carbapenem has decreased activitiy against Pseudomonas?
Ertapenem
What is Cilastatin? What antibiotic is it given in conjunction?
It blocks DIPEPTIDASE in the renal tubule. It is given with IMIPENEM to allow appropriate urinary concentration.
What antibiotic:
Unique Toxicity: seizures, especially impaired renal function (elders, kidney damage)
Imipenem
What antibiotic:
Gives more frequent diarrhea and can cause biliary “sludge,” --> avoided in infants
Ceftriaxone
Contraindication: inactivated in lung by surfactant, so never use in lung infections
Daptomycin

Main toxicity is toward SKELETAL MUSCLE
Only pencillin not eliminated by the kidney?
Nafcillin
What three areas do pencillins NOT hit?
Prostate
Eye
CNS
Name drug association w/ the following adverse rxns:

1) Skin rash, diarrhea, pseudomembranous colitis

2) Interstitial nephritis

3) Phlbitis, neutropenia

4) Elevated hepatic transaminases, neutropenia

5) Neurologic rxns and abnormal behavior with high doses
1) Ampicillin/Amoxicillin

2) Methicillin

3) Nafcillin

4) Oxacillin

5) PEnicillin
What 4 organsims produce B-lactamases?
1) Moraxella
2) Bacteroides
3) H Flu
4) B lactamase producing staph
What aminoglycoside has super high nephrotoxicity? Administration of the drug and its main use?
Neomycin

Before bowel surgery

Only given orally, while other AGs are given IM or IV.
What is the DOC when a bug gentamicin resistant organisms are likely? Why?
Amikacin b/c it's the least susceptible to inactivating enzymes
MOA of AGs?
Inhibit formation of initiation complex by binding to 30S subunit and causing MISREADING of mRNA
-Require O2 for uptake (therefore it sucks against anaerobes)
-Require certain pH level
When do you use spectinomycin?
Uncomplicated gonooccal infections when penicillinase producing organisms are known or suspected
This drug is a 2nd line drug for tx of multi-drug resistant TB
Streptomycin
Three main toxicities of AGs?
NOT
Nephrotoxicity
Ototoxicity
Teratogen
Name 6 organsims that are susceptible to gentamicin, tobramycin, and amikacin
KEEPPS
Klebseilla
E. coli
Enterobactera
Pseudomonas
Proteus
Serratia
Severe gram negative ROD infection
AGs
What are notorious for affecting the absorption of tetracyclines?
Milk, antacids, multivalent cations (calcium, iron, and aluminum).

-Does not affect Doxycyline
MOA for tetracycline
Binds to 30S subunit and prevents attachment of AMINOACYL-TRNA TO THE MRNA RIBOSOMAL COMPLEX
What specifically is doxycycline the DOC?
Drug resistant falciparum malaria
5 toxicities for tetracycline
1) Brown, discolored teeth
2) GI upset
3) Contra in women and kids
4) Pre-renal azotemia
5) Photosenstivity - Doxycycline
Mec of resistance to tetracycline?
Plasmid-coded efflux protein pump
Name tetra's clinical usage
VACUUM THe BedRoom
Vibrio Cholera
Acne
Chylamadia
Ureaplasma Urealyticum
Mycoplasma

Tularemia
H. pylori

Borrelia burgordorferi
Rickettsia

Plus CHANCROID (hemophilus ducreyii)
What two situations would you give somoene tigecycline?
1) Complicated skin and soft tissue infections where resistant organisms known/suspected

2) Complicated intra-abdominal infections
1) Complicated skin and soft tissue infections where resistant organisms known/suspected

2) Complicated intra-abdominal infections
Tigecycline

-Works against MRSA and VRE, but inactive against Pseudo and Proteus
Works against MRSA and VRE, but inactive against Pseudo and Proteus
Tigecycline
What antibiotic would you give when someone is allergic to pencillins and has a Staph or Strep infection?
Erythromycin
DOC for gastroparesis
Erythromycin
Bad taste in mouth is #1 side effect
Clarithromycin
-Also contra in pregnancy
-also treats atypical mycobacterial infections (MAV)
This oral agent has a long half life (3 days)
Azithromycin
Name the extra bugs Azithromycin hits on top of what Clarithromycin hits
H. flu
Moraxella
Chylamydia infections
Mycobacterium avium-intracellulare
Much more active against Strep pneumoniae and Enterococcus faecalis
Telithromycin
-Serious hepatotoxic
Telithromycin's two main uses but main side effect?
More active against Strep pneumonaie and Enterococcus faecalis

Hepatotoxic
Three drugs to treat anaerobic infections
Clindamycin
Metronidazole
Chloramphenicol
What Strep is usually resistant?
Strep Enterococci (at least in the ribosomal agent lecture)
Main toxiciticity for clindamycin?
Pseudomembranous colitis
Applied for staph and strep infections (impetigo)

Where does it come from?

Another use?
Mupirocin

Comes from Pseudomonas fluorescens

Nasal application to eliminate Staph aureus (esp., MRSA) carriage
Treats VRE, MRSA, VRSA, PRSP
Linezolid

Better than Vancomycin for MRSA pneumonia and soft tissue infection

Also treats all staph, strep, and enterococci
MOA of Rifaximin?

Its two main uses? What is it not effective towards?
Binds to beta subunit of the RNA pol to inhibit RNA synthesis

1) Traveler's diarrhea
2) Hepatic encephalopathy

-It's ineffective against Campylobacter jejuni
How do bugs become resistant to chloramphenicol?
Produce a drug inactivating enzyme called CHLORAMPHENICOL ACETYLTRANSFERASE
3 main uses of chloramphenicol?
Meningitis (SHiN organisms

Brain abscesses

Typhoid fever
MOA of chloramphenicol?
Bind to the 50S subunit and inhibits PEPTIDYL TRANSFERASE
3 major toxicities of chloramphenicol
1) Bone marrow suppression

2) Aplastic anemia

3) Gray Baby Syndrome: abdominal distention, cyanosis, circulatory collapse b/c infants can't conjugate chloramphenicol
Bacteria can produce a methylase that confers resistance to what 3 drugs?

How else can they become resistant?
Macrolide
Lincosamide
Strepogramin

They can also change their receptor structure thru methylation. I guess it's the same thing then
Bacteria can produce drug-inactivating enzymes for what two drugs??
AGs
Chloramphenicol
In general, what class of antibiotics are good except for Pseudomonas, but all are excellent drugs for “hospital-acquired” gram-negatives.
3rd gen cephalo
Frequently to treat staphylococcal osteomyelitis

plus another drug that can treat as well
Clindamycin

Ciprofloxacin
Two main classes to treat gram negative infections? Which one avoids nephrotoxicity?
1) AGs

2) Aztreonam (avoids nephro risk and little cross allergenic w/ pencillins and cephalosporins)
“Ultimate” broad spectrum antibiotics
Imipenem (drug of choice for ENTEROBACTER), Meropenem, Doripenem and Ertapenem
The markedly broad spectrum of imipenem predisposes patients to what?
colonization/infection with resistant organisms (such as MRSA or Candida) because of the elimination of normal flora.
MOA of Sulfonamides?
Static!

Interferes with microbial folic acid synthesis by COMPETITING WITH PABA for incorporation into dihydrofolic acid
What two drugs are used to treat nocardiosis?
Sulfanomides with Trimethoprim
What two drugs are used to treat Toxoplasmosis?
Sulfa with Pyrimethamine
4 main toxicities of Sulfa?
1) Displaces other substances from ALBUMIN (ex is bilirubin in neonate so can cause KERNICTERUS)

2) Crystalluria

3) Rashes

4) Fever
MOA of Trimethoprim?
Static!

Inhibition of bacterial dihydrofolate reductase
-This is the MOA for Pyrimethamine
Mimics folic acid defiency
Trimethoprim
Main is use for UTIs due to MOST common urinary pathogens
Trimethoprim
Sulfa+Pyramethamine treats what two disorders?
Toxoplasmosis
Malaria
MOA of fluroquinolones?
Inhibits bacterial DNA gyrase (fns to maintain negative supercoil of bacterial chromosome)
Milk, antacids, multivalent cations (calcium, iron, and aluminum).inhibit what tow drugs absorptions?
Tetracycline
Fluoroquinolones
Agent of choice for prostatitis
Ciprofloxacin
Good for osteomyelitis and soft tissue infection
Ciprofloxacin
Fluroquinolones variably hinder elimination of what two things?
1) Theophyllnes
2) Caffeine
What quinolone is "most active" against Strep pneumo
Moxifloxacin
MOA of Metronidazole
Nitro group of metronidazole is REDUCED by electron transport proteins, making it an "electron sink" and deprives the bacterial cell of required reducing equivalents

-CIDAL action against ANAEROBIC bacteria
Treats anaerobic infections of all types including brain abscesses
Metronidazole
Also can use chloramphenicol (good for anaerobes and for brain abscesses if cannot use other agents)
This drug might cause acute allergic pneumonitis or severe polyneuropathies. What is its clinical use as well?
Nitrofurantion

Used to treat uncomplicated, non-server UTIs
What two huge toxicities are of concern in using Nitrofurantion?
Acute allergic pneumonitis
Severe polyneuropathies
What pencillin is not elminated by the kidney?
Nafcillin

The natural and many extended spectrum penicillins require dosage change in renal insufficiency, as does methicillin.
What treats Enterococcus faecalis?
Penicillin w/ AG
Penicillin is used for tx for what 5 things?
1) STREP INFECTIONS! (Gropu A strep, pneumoniae and ENTEROCOCCUS FAECALIS)

2) Syphilus

3) Neisseria meningitides

4) Many ANAEROBES other than Bacteroides like Clostridia

5) Proven non-pencillinase producing Staph aureus
Name as many pencillinase resistant penicillins?
Methacillin
Nafcillin
Dicloxacillin
Cloxacillin
Oxacillin
Name extended spectrum pencillins and what bugs they own
Amoxicillin
Ampicillin

Amp HELPS kill enterococci

HELPS =
H flu
E coli
Listeria
Proteus
Salmonella
enterococci
What two drugs are very commonly used antibiotics to treat community acquired infections” involving respiratory tract
Ampicillin
Amoxicillin
Extended spectrum pencillins with B lactamase inhibitors generally hit what two organisms?
1) Pseudomonas
2) Enterococcus faecalis

Amoxicillin or Ampicillin with Clauvanic acid or Tazobactam
Adverse reaction: Neuromuscular irritability, including seizures with high doses or renal
failure is for what drug?
Penicillins
What is a side effect for adding a beta lactamase inhibitor?
Increases diarrhea
mainly upper and lower resp. infections (otitis media, sinusitis, bronchitis) where beta-lactamase producing H. flu or Moraxella are expected.
Amoxicillin + Clav acid
very broad
spectrum activity allows them to be “ok” therapy for a wide variety of infections but usually a narrower spectrum agent may be preferable and have greater activity.
Ticarcillin/clavulanic acid and piperacillin/tazobactam
What are possible sources for an expert’s proper factual basis? (3)
[1] personal observation;

[2] facts made known to the expert at trial (hypos);

[3] facts not known personally but supplied to him outside the courtroom and of a type reasonably relied upon by experts in the particular field (ex: Dr. relies on x-ray tech’s opinion of x-ray)
DOC for pseudomembranous colitis from C. diff?
Vancomycin
What class of drugs do you use just for staph?
Very narrow spectrum pencillins
Methacillin
Nafcillin
Dicloxazillin
Oxacillin
Cloxacillin
Red neck” syndrome
erythema, itching, hypotension especially when drug is infused too rapidly. Vancomycin must be given slowly over 60-120 minutes.
What local anesthetic has cardio toxicity? Which causes methohemoglobinemia? Tx?
Cardio = Bupivacaine

Methohemoglobinemia = Prilocaine
-Tx: Methylene blue
Name two incretins and their function

What is the fn of Amylin?
GIP
GLP-1

1) Stimulate insulin secretion
2) Suppress glucagon secretion
3) Slow gastric emptying
4) Increase B cell mas

Dipeptidyl-peptidase, DDP-4 breaks down GLP-1

Amylin: cosecreted with insulin and it serves to reduce excess glucagon secretion in postprandial period.
Name 3 short acting, 1 medium and 2 long acting insulin forms
Short - good for right before a meal b/c of rapid onset. Can cause HYPOglycemia if the meal is delayed.
Lispro
Aspart
Glulisine

Intermediate: supposed to mimic basal insulin levels, but it doesn't as there are a ton of peaks and variable absorption
NPH

Longacting
Detemir: most consistent response with each dose
Glargine: gradual release pattern from injection site
What is the best long acting insulin, i.e. the MOST CONSISTENT response w/ each dose?
Determir
Glargine and Determir are better than NPH. What is their main disadvantage compared to NPH?
They cannot be mixed with other insulins in the same syringe whereas NPH can so there would be more injections with Determir and Glargine
MOA of Glargine
Substituted 2 AAs with Arginine and you inject GLARGINE as an acidic solution (pH 4) into subQ tissue that is pH 7.4 and it precipitates/dissociates slowly. This is how you get an extended time of action
MOA of Determir
They add a fatty acid chain to insulin

The FA allows it to bind to ALBUMIN, which delays distribution of insulin to target tissues
Analog of amylin?

MOA?
AE?
Advantages?
Pramlintide

It is an analog of amylin so it will reduce excess glucagon secretion and also makes you feel full.

AE: NAUSEA

Adv: reduces A1C really well w/ less insulin used and also reduces weight
Name two classes of insulin secretagogues and the drugs in each of those classes

MOA?
Sulfonylureas
Glyburide, Glipizide, Glimiperide
Meglitinides
Repaglinide

MOA: they act like ATP that is produced from glycolysis and CLOSE the K+ channel so the cell gets depolarized, which signals Ca2+ channels to open. A rise in intracellular calcium triggers INSULIN secretion
-B cells are required to be functional for this to work
DNA nucleocapsid viruses (3)
Adeno
papillo
parvo
Why would you use a meglitinide vs. a sulfonyurea?
Meglitinides (Repaglinide) do not release insulin in the absence of glucose
-Can be used in renal insufficiency or hepatic dysfunction
-Lower risk of hypoglycemia
Name 2 alpha-glucosidase inhibitors

MOA?

AE?

Why don't pts use this that much?
Acarbose and Miglitol

Delays digestion of ingested carbs so taht there is a smaller rise in blood glucose

AE: FLATULENCE

Must be taken right before each meal so they tend to not be so compliant
MOA of Metformin?

Main advantages?

Main AE? CI (3)?
MOA: insulin sensitizer so taht there is an increase response to insulin so less hepatic glucose is made

Advantages:
1) Promotes weight loss
2) Reduce LDL and TG
3) Only diabetes drug that protects CV risk
-DOC for DM II

AE: Lactic acidosis

CI: renal failure, liver failure, CHF
Name 2 Thiazolidinediones

MOA?
AE?
CI?
Clinical use?
Rosiglitazone and Pioglitazone
MOA: binds to nuclear PPARy receptor and this augments insulin and also increases GLUT 4 transporters

AE: Edema, Pulmonary edema, WEIGHT GAIN

CI: Liver failure

Clinical use: reduces A1C, drops BP, and B cell preservation
What diabetes drug causes edema, pulmonary edema and weight gain
Glitazones
Rosiglitazone
Pioglitazone
MOA of Exenatide

Advantages?
It is a peptide that binds to GLP-1 receptors but it is resistant to DPP-4

You do not need to monitor glucose levels w/ this drug
It promotes weight loss both short and long term
Preserves B cells and thus reduces A1C
You do not need to monitor glucose levels w/ this drug
It promotes weight loss both short and long term
Preserves B cells and thus reduces A1C
Exenatide
This drug is a GLP-1 analog but they add a FA to it like Determir to increase its half life
Liraglutide
Why would you use Sitagliptin instead of Exenatide?
It is available orally so no injection

Sitagliptin works by blocking DPP-4 so GLP-1 doesn't get broken down
What two molecules make up T4 and then T3? Which one is more potent?

Where is T4 made? T3?
T4 = DIT + DIT
-100% made in the thyroid
-it is less potent than T3

T3 = DIT + MIT
-20% is made in the thyroid gland, but 80% is converted in the peripherally from T4 to T3

Both are highly protein bound
What is the biological significance and regulatory significance of TBG and free thyroid hormone?
Only free thyroid hormone can diffuse into cells and cause a biologic effect. Also, free hormone can regulate TSH secretion from the pituitary
Name some situations where TBG is increased.

Decreased?
Increased:
1) Estrogen via OCT
2) Pregnancy
HY ones

Decreased:
1) Androgenic steroids
2) Glucocorticoids
3) Salicylates
4) Chronic liver dz
5) Nephrosis
How and where is thyroid hormone metabolized?
T4 and T3 are metabolized in the LIVER via conjugation to glucuronic and sulfuric acid

Excretion thru bile via kidney
Name 4 drugs that can cause hypothyroidism
1) Glucocorticoids
2) Dopamine
3) Levodopa
4) Dobutamine
How do anti seizure meds like phenytoin and carbamazepine affect thyroid levels?
They are enzyme inducers...cause low serum TT4, but normal or elevated TSH.
The low serum TT4 is from them displacing them from TBG so serum free hormone goes up? idk...
What drug partially blocks peripheral conversion of T4 to T3 other than PTU?
Propanolol
Name the two hyperthyroid drugs and give their MOA. One of them has 2 MOAs
Propylthiouracil and Methimazole
They block the synthesis of thyroid hormone by inhibiting the perioxidase system from organification adn coupling rxns
PTU also prevents the conversion of T4 to T3

Methimazole is the agent of choice as it is 10x more potent than PTU and tastes better plus cheaper
Main toxicities of PTU and Methimazole? Which one black box?
Rash
Agranulocytosis
Black blox = hepatotoxic (do LFTs; methimazole had less cases vs. PTU in one study)
Absolute contra for Radioactive iodine?
PREGNANCY!
What can you give for a short amt of time before a thyroidectomy?
Iodine - inhibits hormone release and production
Name PTH's actions on the gut, kidney and bone
Gut: increases ca and phosphate intake in teh gut

Kidney: decreases ca, but increases phosphate excretion
-The mec for this is that PTH activates Vitamin D and Vitamin D increases both ca and phos levels

Bone: increases ca and phosphate release from bones
What is Teriparatide?
MOA?
Indication?
Contra?
Recombinant PTH used for osteoporosis by acting on PTH receptors

Contra: Hypersensitivity
What is the plant and animal form of Vitamin D?

What organ is involved in the first step of Vit D synthesis? Second organ?
D2 = Ergocalciferol = Plants

D3 = Cholecalciferol = Animals

Liver = 25 hydroxyvitamin D
Kidney = 1,25 hydroxyvitamin D
What is Calcitriol?
What indication?
Toxicitiy?
Contra?
It is ACTIVATED VITAMIN D used to treat Secondary Hyperparathyroidism due to chronic renal failure. The kidney can't make Vit D so there is no negative feedback on PTH.
Calcitriol will negatively feedback on PTH and decrease it.

Toxicity: Hypercalcemia, Hyperphosphatemia, Hypercalciuria

Contra: Hypercalcemia, Vitamin D toxicity
What is unique about Doxercalciferol?
It is 1 alpha hydroxylated already, i.e. it is a prodrug. It doesn't need the kidney so good for kidney failure patients. It just goes to the liver and this can be used to treat secondary hyperparathyroidism
Prodrog = 1 alpha OH D2

What drug?
Doxercalciferol
What drug is more specific than Calcitriol and so more selective on hyperaparthyroidism?
Paricalcitol

Less vitamin D toxicity
Bypasses kidney function and has less vitamin D toxicitiy

Name two other drugs that bypass the kidney
Paricalcitol

Calcitriol & Doxercalciferol
This drug is the most specific for secondary hyperparathyrodism

What is its main toxicity? MOA?
Cinacalcet

Seizures

MOA: increases the sensitivity of the Ca2+ sensing receptors to free Ca2+, which in turn lowers PTH output
What drug to treat Paget's Dz? What is Paget's Dz? MOA of this drug and other indications (2)?

How is it administered?
Calcitonin is from salmon and NASAL SPRAY

Indicated for Pagets, Osteoporosis and Hypercalcemia

Paget's Dz: enlarged and deformed bones and bone pain caused by excessive and disorganized bone remodeling

MOA: ANTAGONIZES PTH...basically inhibits Ca2+ release from bone
Cancer-associated hypercalcemia is treated w/ what drug?

MOA?

Side effect?
Prednisone
Antagonizes Vi D

Retards bone growth in kids and induces osteoporosis in adults
What suffix do bisphosphanates end in?

MOA?
"Onate"
Alendronate, pamidronate, risedronate...

High affinity for the site of bone resorption, blocks TO of hydroxyapatite
BASICALLY, THEY INHIBIT OSTEOCLASTS
What drug has erosive esophagitis and osteonecrosis of the jaw?
Bisphosphonates

Used for osteoporosis, Pagets, bone metastasis related hypercalcemia.
Two toxicities of bisphosphonates?
Erosive esophagitis

Osteonecrosis of the jaw
What drug to give to a woman who is post menopause and has osteoprosis?

Side effect? MOA?
Raloxifene
Selective E receptor modulator (SERM) that is AGONIST on BONE, but ANTAGONIST on breast and uterus

Hot flases and leg cramps
Drug for hyperpohpsphatemia? MOA?
Sevelamer

Chelates/sequesters dietary phosphate in food
What diuretic increases Ca excretion? decreases?
Furosemide = increases excretion

Thiazides decrease excretion and can actually cause hypercalciuria
What are Gallium nitrate and Plicamycin used for?
Gallium nitrate: cancer related HYPERcalcemia and also inhibits osteoclast

Plicamycin: malignant tumors of the tests and inhibit RNA synthesis of osteocalsts
What drug for malignant tumors of testis?
Plicamycin

Gallium nitrate:cancer related HYPERcalcemia
What drug is best for class 2 anovulation?

MOA?
Clomiphene citrate
-Works by blocking the E receptors on the hypothalamus and pituitary thereby eliminating negative feedback and a stimulation to release FSH and LH and so enhances folliculogenesis and steroidogenesis

Class 2 is when there are normal GnRH levels, but the follicular phase is suboptimal
-MCC of infertility
How is Metformin used for infertility?
Metformin is used as an insulin SENSITIZER and often used to treat polycystic ovarian syndrome, which is a cause of anovulation.
Follitropins
MOA?
Adverse rxns?
MOA: increases folliculogenesis, maturation of the follicle and gonadal steroid production

Adverse rxns: HA, ovarian cysts, ab pain, nausea, ovarian hyperstimulation
inhibition of a microorganism by a substance actively produced by another microorganism.
Antibiosis-
what drug can cause acute interstitial pneumonitis?

what can cause esophageal ulcers?
Nitrofurantoin

Doxycycline
3 potential offenders of infertility
EtOH
Caffeine
Smoking
Distinguish b/t the 3 classes of infertility
Class I = HYPOgonadotropic hypogonadal anovulation = low FSH and estriadiol conc b/c of GnRH or pituitary unresponsiveness to GnRH

Class 2 = Normogonadotropic normoestrogenic anovulation = Normal GnRH and E, but the FSH secretion is SUBOPTIMAL during follicular phase
-Polycystic Ovary Syndrome

Class 3 = Hypergonadotropic hypoestrogenic anvolution = premature ovarian failure (premature menopause) = E is low, but hypothalamus levels are regular or elevated b/c E is NOT feeding back
Polycystic ovary syndrome causes what class of anovulation?
Class 2
What is the MCC of Cushing's syndrome?
Pituitary adenoma
What is hte tx for Cushing's syndrome?
Surgery
Pharmacological therapy is 2nd line and usually just adjunctive b/c they are pretty toxic
-Basically use while waiting for surgery or radiation therapy
Mitotate
MOA?
What is its goal? How long are you supposed to use it? AEs?
MOA:
1) Inhibition of steroid synthesis
2) Alteration of peripheral steroid metabolism
3) Inhibition of adrenal cortisol release

Goal is to completely ablate cortisol production. Use it for 6-9 months

AE:
1) GI = Nausea/Anorexia/Diarrhea
2) Neuromuscular = Fatigue/muscle weakness with CNS depression
Name 1 steroidogenic inhibitor, 3 adrenal enzyme inhibitors and 1 glucocorticoid antagonist
Steroidogenic = Mitotate

Adrenal Enzyme Inhibitor
1) Aminoglutethimide
2) Metyrapone
3) Ketoconazole

Glucocorticoid antagonist = Mifepristone
What Cushings tx causes drug induced lupus?
Aminoglutethimide

also causes bone marrow suppression and drowsiness
MOA of aminoglutethimide?
Inhibits desmolase
MOA of Metyrapone?
Inhibits 11B-hydroxylase (last step to get to cortisol)

AE causes increase of other adrenal hormones --> acne, edema, hirsutisim, hypokalemia, lightheadedness
MOA of Ketoconazole?

AE?
MOA
1) Inhibits 17 alpha hydroxylase
2) Inhibits 11 beta hydroxylase
3) Inhibits desmolase
4) Potent inhibitor of T
-All done at high doses of the drug

Increase LFTs, gyncomastia, decreased libido, impotence
-MONITOR LIVER ENZYMES!
MOA of Mifepristone?
Glucocrticoid and Progesterone antagonist. Cortisol levels are not reduced
How much tissue must be lost before you get signs of Addisons? What are some signs?
90% loss of tissue fn before signs and sxs (at least for primary causes), which will also show increase ACTH

Weakness, weight loss, anorexia, nausea, vomiting, ab pain, diarrhea, constipation, hyperkalemia, hyponatremia, hypoglycemia, hypercalcemia, hypothyroidism, salt craving, hyperpigmentation
What drug for cortisol replacement? Mineralcorticoid replacement?
Cortisol = Hydrocortisone or cortisone acetate

Mineralo = Fludrocortisone acetate
What is it when a pt has flu like symptoms initially, then progress to fever, hypotension and shock?

Tx?
Acute Adrenal Insufficiency

Tx w/ hydrocortisone stat
Name the 7 glucocorticoids and their main differences
1) Cortisone
-High mineralcorticoid activity
-Short acting
2) Hydrocortisone
-High mineralcorticoid activity
-Short acting
3) Prednisone
4) Triamicinolone
5) Methylprednisone
6) Dexamethasone
-Very potent anti-inflammatory
-Long acting
7) Betamethasone
-Very potent anti-inflammatory
-Long acting

Triamcinolone to betamethasone have NO mineralcorticoid activity
In terms of hematology, what would you notice in the blood w/ long term use of cortisol therapy?
Lymphocytopenia
Eosinopenia
Monocytopenia

However, neutrophilia

Immune response is inhibited and the inflammatory response as well so increase susceptibility to infection
Agent of choice for anaerobes
Clindamycin
Frequently used for staph osteomyelitis
Clindamycin
What drug should you avoid foods rich i ntyramine?
Linezolid - it is a weak MAO inhibitor and so can cause increased BP and serotonin syndrome w/ antidepressants?
What two organsims is Chloramphenicol generally sucky for?
Sucks for Staph and Pseudomonas

-Good for Strep species and most gram negatives EXCEPT pseudo
What are 4 indications for Strepogrammin usage?
VRE
MRSA
VRSA
PRSP (Penicillin Resistant Pneumococci)
What test do you administer to see if you can discontinue use of corticosteroids?
Cosyntropin Test
-Tapering schedule includes reducing the dose every 1-2 weeks and then adding a short acting agent such as Hydrocortisone or Prednisone.
If you are allergic to sunscreen, what local anesthetic calss should you use?
Use Amino Amides instead (lidocaine, prilocaine, bupivacaine (CV Toxic)
What si the max dose for the following
1) Cocaine
2) Lidocaine
3) Bupivacaine

Also mention duration of action
Cocaine = 1.5-3mg/kg nasally
-Medium duration of action

Lidocaine = 4.5mg/kg w/o Epi and 7.0mg/kg w/ Epi
-30-60 minutes

Bupivacaine = 1.6-2mg/kg w/o Epi and 3mg/kg w/ Epi
-120-240 minutes
What is determines the potency of a local antehestic?

What determines the onset of action?

What determines the duration?
Potency is dependent on lipid solubility; i.e. the more lipid soluble, tehn the more potent

Onset is dependent on pKa. If pKa is closer to body's pKa, then quicker onset of action

Duration is dependent on the strength of the anesthetics binding to protein.
What two anethestics are used for spinal anethesia and epidurals?
Lidocaine
Bupivacaine
Adverse effects of Nitrous Oxide?

Describe it's solubility in blood and lipid and describe what that means
Trapped "air pockets" expand when N2O replaces N2 and this can cause severe pain

Low lipid and blood solubility = not very potent, but fast induction and recovery
Adverse effects of Halothane?

Describe it's solubility in blood and lipid
"Halothane hepatitis" is from repeated exposure to Halothane. The agent can be severely hepatotoxic.

High lipid solubility and high blood solubility = highly potent, but slow onset of action and slow recovery
Hyperthermia, muscle rigidity, tachycardia, and hypercapnia. What is wrong? Tx?
Malignant hyperthermia = caused by all general anesthetics.
-It is usually caused by concominant usage of inahlational anesthetics w/ succinylcholine.

Tx = stop the drug and give Dantrolene
What is great about Isoflurane?
It's widely used!

It has low blood solubility so fast onset and fast recovery
It's also a great muscle relaxant and does not sensitize the heart to catecholamines

The key point: DOES NOT PRODUCE SEIZURE LIKE EKG ACTIVITY!!!!!!!!!!!!!!!!!
What are 3 general systemic effects of inhalational anesthetics? Be sure to include exceptions to the rules
1) Reduce BP, CO, TPR
2) Reduce RR (exception is NITROUS OXIDE)
3) Enhance hearts rxn to catecholamines (exception is Isoflurane) Halothane>Enflurane>Isoflurane)
What is thiopental's main use? Why?
It's main use is INDUCTION of anesthia b/c it gets redistributed throughout other body compartments so it doesn't last very long.
What drug do you use for anesthia induction and/or maintenance?
Propofol
MOA of Praziquantal?
Increases calcium permeanbility and the increase ca++ uptake induces a tetanic state and severe muscular contraction
MOA of Benzimidazoles?
Inhibition of microtubule assembly and BLOCKAGE OF GLUCOSE UPTAKE
DOC for Strongyloides?
THIAbendazole
DOC for cysticercosis?
ALbendazole
MOA for Metronidazole?
Prodrug that is taken up by protozoa and ANAEROBIC bacteria and converted to FERREDOXIN, which disrupts DNA helical structure and inhibits nucleic acid synthesis
What anti-protozoal agent is contra in 1st trimester of preg?
Mebendazole
What drug interaction exists for Mebendazole? What happens?
Carbamazepine lowers plasma levels of Mebendazole
How are tetracyclines eliminated? Exception?
metabolized by liver, excreted via the kidneys.

Doxycycline is excreted in the feces though. Therefore, you can still give Doxycycline to renal failure patients.
Due to this side effect of Linezolid, what should you monitor?
Linezolid can cause THROMBOCYTOPENIA and neutropenia and so you MSUT MONITOR BLOOD COUNTS!
Refractory C. diff infection

Tx?
Rifaximin
if a patient has meningitis, but IV treatment is not feasible, what oral drug can you give?
Oral chloramphenicol
Treating a patient and you notice a rise in the iron count, what drug did you just give them?
Chloramphenicol - it decreases the incorporation of iron into hemoglobin and that's how it causes anemia
What is first line for mild symptoms of GERD?
Antacids b/c it neutralizes the acid, but it also has "SOME INCREASE IN LES TONE"
When would H2RA be better than PIs in teh tx of GERD?
H2RA decrease BASAL acid secretion so it could help a guy who experiences GERD at night time.

PPIs only work when the proton pump is activated or triggered by a meal
MOA of Metoclopramide?

Why would we give thsi drug?
It's used for GERD b/c it can ACCELERATE UPPER GI MOTILITY/EMPTYING WITHOUT stimulating gastric secretion

-It also increases persistalsis of the gastric antrum, duode. and jujun.

Blocks DA receptors (caution in Parkinson's pts)
What pts are contra for use of Bethanecol?

MOA?
Asthma/COPD
and
PUD

Stimulates cholinergic receptors which causes an increase in GI motility and LES tone so can relieve symptoms of reflux

Note: Bethanecol and Metoclopramide are to only be used as ADJUNCTIVE AGENTS with anti-secretory agents
What is the most POTENT inhalational anesthetic?

What two sideeffects?
Methoxyflurane

Can casue arrythmias
and also NEPHROTOXIC via metabolite
Dissociative anesthia means what?

What drug does it apply to?
The patient is non-communicative, but they may move and seem awake

Ketamine
-Excellent analgesia
-Limited usefulness due to CV stim and high incidence of re-mergence hallucinations
Re-emergent halluciations
or
High incidence of delerium following emergence or bad dreams
Ketamine
Induction and maintenance of anesthia
Propofol
What anesthetic can cause Addison's crisis?

When is it primarily used?
Etomidate

Used primarily when at risk for HYPOtension
Slide on relative effects of injectiable hypnotics and anesthetics

Barbituates vs. Opioids vs. BZDs vs Ketamine

Which are good for hypnosis, analgesia and amnesia?
Barbituates
-Hyponosis

Opioids
-Good analgesia

BZDs-
Unpredictable hypnosis (barbituate is good for hypnosis)
-Excellent AMNESIA

Ketamine
-Good hypnosis
-Excellent analgesia
-Good amnesia
What type of peripheral nerve is most susceptible and least susceptible?
Most susceptible are small and myelinated fibers!
-Sensory is also easier than motor
What form of the sodium channel do local anesthetics have a higher affinity for?
Local anesthetic agents have a higher affinity for the channels in an OPEN or ACTIVATED FORM than the resting form
What dose adding a vasoconstrictor do in terms of anesthesia?
It will constrict vessels and prevent toxicity

HY!
What is the difference between ester metabolism and amino amide metabolism?
Ester
-Hydrolysis by plasma cholinesterases

Amide
-Metabolism by microsomal enzymes located primarily in the liver
-Slower than ester local anesthetics
-Systemic toxicity more likely
Difference between laxative, cathartic and purgative
Laxative - mild effect (soft, FORMED stool over a period of hours or days)

Cathartic - more intense effect (more prompt and "fluid"

Purgative - VERY intense effect w/ a lot of pain and cramping
Name the 4 bulk forming laxatives
1) Dietary fiber

2) Methylcellulose

3) Psyllium

4) Polycarbophil

*Psyllium and polycarbophil have bloating and flatulence as common side effects
Two drugs have the following MOA

-Inhibit the absorption of water and stimulate perstaltic movements
Bisacodyl

Senna/Sennosides
MOA of Bissacodyl

Senna/Sennosides
Inhibition the absorption of water

Stimulate perstalsis
MOA of Caster Oil
Castor oil is hydrolyzed in the SI to release RICINOLEIC ACID, which acts to inhibit the absorption of fluid and stimulate perstalsis (like Senna/Sennosides or Bisacodyl)

-It can cause complete evacuation so it is used to prepare the bowel for diagnostic procedures sometimes
Two osmotic laxatives
Magnesium hydroxide

Polyethylene glycol - widely used as a general laxative and to prep for diagnostic/surgical procedures
-Do not use osmotic laxatives for chronic use due to their intesne and thorough effects
What is the risk of mineral oil (3)?
It lubricates your crap

1) Oil leaks out your butt and stains furniture

2) Decrease absorption of vit. ADEK and fat soluble drugs

3) Risk of LIPID PNEUMONITIS from aspiration of oil
MOA of Docusate sodium
Exerts a DETERGENT EFFECT to break and soften the fecal mass
MOA of Lubiprostone
Activates chloride channels on the intestinal brush border and thereby increase fluid secretion

-Few systemic effects
Opioid analog

Anti-diarrhea

No CNS effects
Ioperamide
MOA of Ioperamide?
Opioid analog and so decreases perstaltic movement (opioids cause constpiation)

There is also a low abuse potential with Ioperamide and are avaialble OTC
Name the two anticholinergic agents used for anti-diarrhea

What are they mainly used to treat?
Propantheline

Dicyclomine

Irritiable bowel syndrome (alternating diarrhea/constipation caused by stress and anxiety)
Drug to avoid in pediatric population and that has diarrhea? Why?

What else happens to the stool?
Colloidal bismuch compounds (contain citrate and salicylate, Pepto-Bismol)

Darkens the color of stool

Bismuth subsalicylate is contra for kids at risk for Reye's
If pt is allergic to aspirin, what anti-diarrhea drug can you NOT give?
Bismuth subsalicyte

MOA: absorbs excess water and can also bind to some microbial toxins
MOA of Sulfasalazine
Sulfasalazine is converted to sulfapyridine and aminosalicyclic acid.

Aminosalicylic acid has anti-inflammatory activity and improves sx in pts w/ mild/moderate ulcerative colitis
Two drugs to treat UC
Sulfasalazine

Mesalamine
MOA of Infliximab

Used to treat what?
Monoclonal antibody that binds and inactivates the cytokine TNF-alpha and suppresses immune function

Crohn's Dz
Two uses for Bethanechol
1) Treat postoperative ileus (bowel obstruction)

2) Increase LES tone (GERD)

Cholinergic agonist = cramping, diarrhea, salivation, sweating, urinary incontinence, etc.)
Two uses of Simethicone
1) Antigas and anti-flatulent action

2) Prevents large gas bubbles from forming
What diabetes drug has a lot of drug-drug interactions?
Saxagliptin
-Inhibits P450
-MOA: inhibits DPP-4, which breaks down GLP-1
Two drugs that can be used to control GI varices
Desmopressin
Vasopressin

-Used typically for bedwetting control, polyuria from DI or head trauma

-Potent vasoconstrictors
-Promotes clotting factors
Which abx has no cross resistance with otehr drugs?
Linezolid
Post menopausal osteoporosis
Raloxifen (SERM)
3 drugs for cancer related hypercalcemia
1) Prednisone
2) Bisphosphonates
3) Gallium nitrate
Two drugs for Pagets
1) Calcitonin
2) Bisphhosponates