Pharm Flashcards by Lindsay Robinson

What class of diabetic drug?

binds to an intracellular nuclear receptor, PPAR-y (peroxisome proliferator-activated receptor-gamma).

acts as a transcriptional regulator of many genes involved in glucose and lipid metabolism

improves insulin sensitivity

Thiazolidinediones (pioglitazone)

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Treatment for Arsenic poisoning (hypotension, garlic odor on breathe)

-insectisides, contaminated water

Dimercaprol (i.e. British Anti-Lewisite) increases urinary excretion of heavy metal

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adverse reaction to antipsychotic meds (i.e. given during manic episodes)

Neuroleptic Malignant Syndrome (NMS) = hyperthermia (fever), msucle rigidity and confusion

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a first-line Tx for alcohol use disorder

-blocks the rewarding and reinforcing effects of alcohol and shown to reduce craving for it

Naltrexone (Opioid antagonist)

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a selective phosphodiesterase (PDE)-3 enzyme inhibitor the decreases the rate of degradation of cAMP in cardiac tissues

an inotropic (contractility) agent for pts with refractory heart failure d/t left ventricular systolic dysfunction

increased cAMP promote Ca++ influx into cardiac myocytes = inc contractilty

increased cAMP in vascular smooth muscle cells = systemic vasodilation = dec BP = hypotension

Milrinone

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directed against the CD20 antigen (B-cell marker) and improves the prognosis of some lymphomas (i.e. non-hodgkin’s lymphoma)

Rituximab

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a monoclonal antibody used in treatment of breast cancer

trastuzumab (Herceptin)

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gonadotropin-releasing hormone agonist that causes a transient increase in pituitary LH secretion, leading to rise in testosterone levels (DHT mirrors testosterone levels)

HOWEVER, continuous use suppresses LH release and leads to a decrease in testosterone production.

used for prostate cancer

Leuprolide

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A peripheral blood smear has multiple, small rings called trophozoites and banana-shaped gametocytes suggesting Plasmodium infection (malaria).

To treat erythrocytic forms of parasite?

required to kill P vivax and P ovale dormant liver forms (hypnozoites)?

chloroquine and mefloquine

Primaquine

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used to treat onchocerciasis (river blindness)

Ivermectin

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selective cyclooxygenase 2 (COX 2) inhibitor

relieves pain with lower risk of bleeding and gastric ulceration (peptic ulcers)
have been associated with inc risk of Cardiovascular events (bc normally Cox 2 produces prostacyclin which has anticoagulant and vasodilatory actions)

Celecoxib (Cele-tive cox inhibit)

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binds to FK-506 binding protein (FKBP) in the cytoplasm of a T cell.

complex binds and inhibits mTOR blocking IL-2 signal transduction and preventing cell cycle progression and lymphocyte proliferation.
immunosuppressive agent

Sirolimus

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reversibly inhibits a critical step in de novo purine nucleotide synthesis (inosine monophosphate dehydrogenase) which is required for proliferation of activated lymphocytes

selectively targets lymphocytes, reducing B and T cell proliferation and Ab production while promoting T cell apoptosis
immunosuppressive

Mycophenolate

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What TYPE III Hypersensitivity Rxn to nonhuman proteins can occur following administration of chimeric monoclonal antibodies (RituXImab adn InfliXImab)?

Serum Sickness - fever, pruritic rash, arthralgias (joint pain), small vessel vasculitis (fibrinoid necrosis and neutrophil infiltrate)

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What drugs can be used to control severe Graves’ ophthalmopathy?

-decreases severity of inflammation and decreases extraocular volume

High-dose Glucocorticoids (prednisone)

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what 2 drugs inhibit thyroid peroxidase, thus reducing iodine organification?

Methimazole and Propylthiouracil

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Direct arteriolar vasodilators lower BP but the effect is limited by subsequent stimulation of baroreceptors with resulting reflex sympathetic activation (RAAS, inc. heart rate, contractility, CO).

tachycardia
Na+ and fluid retention - edema

Hydralazine

Minoxidil

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Name 3 antibiotics commonly used for invasive methicillin-resistance Staphylococcus Aureus infections.

Vancomycin
Daptomycin
Linezolid

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antibiotic that blocks glycopeptide polymerization by binding tightly to D-alanyl-D-alanine inhibiting bacterial cell wall synthesis

1st line Tx for MRSA

S/E: Red man syndrome, nephrotoxicity

Vancomycin

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antibiotic that depolarizes cellular membrane by creating transmembrane channels inhibiting DNA, RNA and protein synthesis

limited to gram+ organisms ONLY (MRSA)

S/E: myopathy & CPK elevation

NOTE: inactivated by pulmonay surfactant (ineffective in treating pneumonia)

Daptomycin

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antibiotic that inhibits bacterial protein synthesis by binding to the 23S rRNA of the 50S subunit

S/E: Thrombocytopenia, Optic Neuritis, High risk for serontonin syndrome (esp. if used with proserotonergic drugs - Citalopram)

used for MRSA

Linezolid

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increases circulating factor VIII & endothelial secretion of vWF to stop bleeding (Hemophilia A, vWF Disease)
binds to V2 receptors in renal tubular cells, leading to increased aquaporin channels, increased H₂O reabsorption & decreased urine output (Central DI, nocturnal enuresis

Desmopressin (DDAVP) therapy

synthetic analog of vasopressin (ADH), normally released by posterior pituitary

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an aldosterone antagonist used to treat heart failure, blocking aldosterone’s detrimental cardiac effects

significant antiandronergic effects = gynecomastia, decreased libido, impotence

S/E: hyperkalemia

Spironolactone

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more selective aldosterone antagonist with fewer side effects

Eplerenone

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**Topical prostaglandin** that **increases outflow of aqueous humor** via the uveoscleral pathway. ## Footnote **Preferred Tx for Open-Angle Glaucoma**

Latano**prost**

**First-generation antihistamines** are designed to relieve the allergic symptoms caused by histamine release from mast cells (rhinorrhea, itchy eyes/nose, urticaria). However, they **also have antimuscarinic**, **anti-alpha adrenergic**, **anti-serotonergic properties**. Therefore, **AVOID IN ELDERLY** with cognitive or functional impairments!\*\*\* **Anticholinergic effects on the ocular ciliary muscles impair accomodation and cause blurring vision for close objects (reading).**

**chlorpheniramine, diphenhydramine, hydroxyzine, promethazine**

What drug to give if someone is having an adverse reaction to antipsychotic medications**, Neuroleptic Malignant Syndrome** (muscle rigidity, hyperthermia, autonomic instability (HTN, Tachy), altered sensorium).

**Dantrolene** - used to **reduce muscle rigidity by antagonizing RyR1** receptors **inhibiting Calcium ion release from the SR of skeletal muscle.**

What class of drugs **ameliorate symptoms of thyrotoxicosis** by **decreasing the effect of sympathetic adrenergic impulses on target organs.** It also **decreases the rate of peripheral conversion of T4 to T3.**

**Beta-blockers** (propano**lol**)

What 2 drugs **decrease thyroid hormone synthesis**? What can **limit Thyroid hormone release?**

Propylthiouracil and Methimazole pharmacologic doses of Iodine

15 yo boy has **3 months of periodic, sudden-onset, jerking movements involving both arms** that occurs **early in the morning** neither suppressible nor preceded by an urge (Tourette's) **Best initial treatment for this kid?**

**Valproid Acid (broad-spectrum anti-convulsant --\> Lamotrigine, Levetriacetam, Topiramate)** used for **junvenile myoclonic epilepsy** (form of generalized epilepsy)

Name some **Broad-Spectrum Anticonvulsants** used to treat **Generalized Epilepsy** (Tonic-Clonic, Myoclonic).

1. Lamotrigine 2. Levetiracetam 3. Topiramate 4. Valproic Acid

Name some **Narrow Spectrum anti-convulsants** used to **treat Focal Epilepsy (Simple and Complex)**

1. Carbamazepine 2. Gabepentin 3. Phenobarbital 4. Phenytoin

Name preferred anticonvulsant **used to treat Absence Seizures.**

Ethosuximide

**HIV Drug** a **nucleoside reverse transcriptase inhibitor (NRTI)** competitively binds to reverse transcriptase and is **incorporated in to the viral genome as a thymidine analog** does **not have a 3'-OH group**, **_making 3'-5' phosphodiester bond formation impossible_****\*\*\*\***

**Zidovudine (AZT)**

integration of viral DNA in to the host genome is mediated by **integrase, a retroviral enzyme that is inhibited by** _____________ (an integrase inhibitor)

**Raltegravir**

**Chemotherapeutic agents** that **intercalate between the bases of double-stranded DNA** causing **defective base pairing and splitting of the DNA strands** ## Footnote **anthracyclines**

Daunorubicin and Doxorubicin

\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ are **first-line Tx for acute gouty arthritis**. They i**nhibit cyclooxygenase decreasing PGs synthesis** and **exert a broad anti-inflammatory effect that includes inhibition of neutrophils.**

NSAIDs (naproxen, indomethacin) ## Footnote **Colchicine - secondary line of tx**

**Xanthine Oxidase inhibitors** are used to prevent acute attacks in patients **with RECURRENT AND PROGRESSIVE gouty arthritis** and those with macroscopic tophi. \*\*SHOULD NOT BE INITIATED DURING AN ACUTE GOUT attack bc can exacerbate acute arthritis.

Allopurinol, Febuxostat

Newer-generation antihistamines have minimal side effects. They are less lipophilic, do not readily cross BBB and usually nonsedating.

**Loratadine, Cetirizine**

Name the drug class: Antiobiotic Resistant Mechanism - B-lactamase - mutated PBP - Mutated porin protein

Penicillins

Name the drug class: Antibiotic Resistance Mechanisms - mutated peptidoglycan cell wall (replaces D-alanyl D-alanine with D-alanyl D-lactate) - impaired influx/increased efflux

Vancomycin

Name the drug class: Antibiotic Resistance Mechanism - mutated DNA gyrase - impaired influx/increased efflux

Fluoroquinolones (Ciprofloxacin)

Name the drug class: Antibiotic Resistance Mechanisms -Aminoglycoside-modifying enzymes that transfer diff chemical groups to the AMG Antibiotic molecule decreasing its ability to bind to ribosomes and exert its antimicrobial effects

Aminoglycosides (Gentamicin)

Name the drug class: Antibiotic Resistance Mechanisms - impaired influx/increased efflux - inactivated enzyme - synthesize a protein that allows ribosomes to perform translation even in the presence of the antibiotic

Tetracyclines (MInocycline)

Name the drug class: Antibiotic Resistance Mechanism -mutated RNA polymerase

Rifamycins

an **N-methyl-D-aspartate receptor antagonist;** works secondarily to inhibit the reuptake of NE, Dopa, Serotonin has **dissociative and anesthetic** effects **psychosis and severe agitation** leading to violent trauma **ataxia**, **horizontal and vertical nystagmus**, **delirium**

Phencyclidine (PCP)

**Dopamine agonists** have chemical structure similar to neurotransmitter Dopamine and **directly stimulates dopamine receptors.** **Tx: Parkinson's Disease** 2 Classes of Dopa Agonists: (1) Ergot compounds (2) Nonergot Compounds

**(1) Bromocriptine** (also treats Hyperprolactinemia) ## Footnote **(2) Pramipexole, Ropinirole**

**Tx: Parkinson's** MOA: **decreases central dopamine degradation** via **inhibition of MAO-B in the brain**

Selegiline

Tx: Parkinson's MOA: enhances the effect of endogenous dopamine

Amantadine

Tx: Parkinson's MOA: increase dopamine precursor availability in the brain (decreases breakdown of Levodopa in peripheral tissues) COMT inhibitors: ?? Dopa decarboxylase inhibitors: ??

COMT Inhibitors: Entacapone, Tolcapone Dopa Decarboxylase Inhibitors: Carbidopa

Tx: Parkinson's (tremor as predominant symptom) MOA: inhibits central muscarinic receptors (anticholinergics)

Benztropine

**Treatment for Atropine Poisoning** (dilated pupils, non-reactive to light, flushed skin, dry oral musosa) ## Footnote **gardening**

**Physostigmine (cholinesterase inhibitor)**

**First-line treatment for alcohol withdrawal?** I**f patient has advance liver disease?**

Benzodiazepines (Diazepam or Chlordiazepoxide) w/o active metabolites (Lorazepam, Oxazepam, Temazepam)

Combination insulin therapy includes a basal-bolus combo. Basal insulin given once at bedtime and bolus insulin given multiple times a day with meals. **Mealtime bolus insulin with reversed lysine and proline residues at the C terminal end of the B chain includes... ???**

**Lispro, Aspart and Glulisine (give so you have "NO LAG")**

Long-acting insulin analogs have a flatter and longer action profile.

Detemir and Glargine (longest)

**First-line Tx for Primary syphilis** (Treponema pallidum - gram - organisms with a peptidoglycan cell wall)? **covalently binds to and inhibits transpeptidase** inhibiting the final cross-linking step in peptidoglycan cell wall synthesis **structural similarity to D-alanine-D-alanine**

Penicillins

antibiotic that **directly binds to the D-alanine-D-alanine residues** preventing the incorporation of new subunits in to the cell wall

Vancomycin

**GP IIb/IIIa receptor antagonist that inhibits binding of this receptor to fibrinogen** useful for TX for unstable angina and acute coronary syndrome NOTE: GP IIb/IIIa is deficient or defective in patients with Glanzmann Thrombasthenia

Abciximab

**direct thrombin inhibitor** used in **heparin-induced thrombocytopenia**

Argatroban

**direct thrombin inhibitor** used in **atrial fibrillation or venous thromboembolism**

Dabigatran

potentiates antithrombin III activity leading to inactivation of thrombin and factor Xa

Heparin

prevents K-mediated carboxylation of several coagulation factors

warfarin

COX 1 and 2 inhibitor that inhibits TXA2 release from platelets preventing platelet aggregation

Aspirin

**inhibits platelet aggregation** by **blocking P2Y12 on platelet ADP receptors**

Clopidogrel

**irreversibly bind to bacterial 30S causing mRNA genetic code misreading and inhibiting bacterial protein synthesis** need to diffuse inside the cell to reach the ribosomes so **often prescribed with penicillins or vancomycin** **SE: ototoxicity (tinnitus, hearing loss) and nephrotoxicity**

Aminoglycosides (gentamycin)

act on bacterial DNA gyrase to prevent DNA unwinding

Fluoroquinolones

combo that affects bacterial folic acid synthesis

Trimethoprim-sulfamethoxazole

disrupts bacterial membrane by creating transmembrane channels that cause intracellular ion leage and cellular membrane depolarization S/E: Myopathy and Rhabdomyolysis

Daptomycin

**NON-Nucleoside** Reverse Transcriptase Inhibitors (NNRTIs) antiretroviral drugs that **DO NOT REQUIRE activation via intracellular phosphorylation** acts within the cytoplasms of infected cells **inhibiting the synthesis of viral DNA from the RNA template (inhibiting reverse transcriptase)** **S/E: hepatic failure, life-threatening skin infections (stevens-johnson syndrome)**

**Nevirapine and Efavirenz**

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) must be converted into their monophosphate forms by cellular thymidine kinase before becoming pharmacologically active

Zidovudine and Emtricitabine

an HIV fusion inhibitor that binds to HIV envelope gp41 and blocks the conformational changes necessary for the fusion of virus with host CD4+ T cells acts outside the cytoplasm

Enfuvirtide

an inhibitor of HIV protease that prevents assemby and maturation of the virus non-functional, noninfecting virions are produced instead

Ritonavir, Saquinavir

CCR5 receptor inhibitor (for HIV)

Maraviroc

These medications **reduce hepatic VLDL production and increase LPL (lipoprotein lipase) activity** _LPL_: hydrolyzes triglycerides in chylomicrons and VLDL to release free fatty acids and also transfers these lipoproteins to HDL **decreasing Triglycerides**

Fibrates (Feno**fibrate,** Gem**fibro**zil**)** **Niacin** **Fish Oil (**also inhibit synthesis of apolipoprotein B)

selectively blocks intestinal cholesterol absorption

Ezetimibe

bile acid-binding resins increase fecal loss of cholesterol by binding bile acids in the intestine and disrupting enterohepatic bile acid re-circulation

Chloestyramine

monoclonal antibodies that reduce LDL receptor degradation in the liver pts with high cholesterol levels

PCSK9 Inhibitors

decrease hepatic cholesterol synthesis by inhibiting HMG-CoA reductase

Statins

**recurrent C. Diff infections** **oral macrocytic antibiotic that inhibits the sigma subunit of RNA polymerase** -leads to protein synthesis inhibition and cell death (Bacteriocidal) **-administererd orally** and minimal systemic absorption resulting in high fecal concentrations

Fidaxomicin

Patient with **Postherpatic Neuralgia applies topical Capsaicin.** This results in **decreased activity of which neurotransmitter** resulting in **pain relief**?

Substance P

Selective Blockage of B₁ adrenergic receptor leads to decreased cAMP levels in cardiac and renal juxtaglomerular tissues. NO effect on vascular smooth muscle.

Atenolol

Nonselective Beta Blocker blocks both B₁and B₂ adrenergic receptors therefore a decrease in cAMP in cardiac myocytes, renal juxtaglomerular cells and vascular smooth muscle will occur.

Propanolol

What drug **inhibits Cholesterol 7-alpha hydroxylase** (rate limiting step in the synthesis of bile acids) resulting in increased risk of **Cholesterol Gallstones?**

Fimbrates (Gem**fibro**zil, Feno**fibrate**)

Most common cause of death in **Tricyclic antidepressant overdose (amitriptyline)?**

cardiac arrhythmias and refractory hypotension d/t inhibition of fast sodium channels in cardiac myocytes

Oral Morphine (opiates) most likely directly effects the spinal cord neurons by doing what? attenuates pain transmission = produces analgesia

Decreased calcium influx at the presynaptic terminals = decreased excitatory neurotransmitter release opening of K+ channels in the postsynaptic membrane = hyperpolarization

**Vancomycin** inhibits what type of bacterial organisms?

Gram + (S. pyogenes, S. pneumoniae, C. Diphtheriae)

**What antifungal?** - **binds the ergosterol of fungal cell membranes** leading to **fungal cell lysis** - also binds cholesterol to some degree causing toxicity to human tissues S/E: **nephrotoxicity**, **hypokalemia**, **hypomagnesemia,** acute infusino-related reactions (fever, chills, rigors and hypotension)

Amphotericin B

**Triazole antifungals inhibit cytochrome P450 enzymes** suppresing the metabolism of many medications.

Fluconazole, Itraconazole

**binding of microtubular proteins** - effective against **dermatophytes ONLY** - antifungal agent

Griseofulvin

Two drugs commonly utilized in combination with aggressive fluid hydration to protect our organs from destruction from **Tumor Lysis Syndrome** (when # of tumor cells destroyed in a short period of time).

**Allopurinol:** i**nhibits uric acid formation during cell lysis** **Rasburicase**: urate oxidase enzyme present in mammals, not humans; **catalyzes the conversion of uric acid to allantoin, a more soluble metabolite for excretion**

What Type II Diabetes drug **decreases insulin resistance by binding to \*\*_PPAR-y_,** **a transcriptional regulator of genes**. Results in **increased GLUT4** transmembrane glucose transporters on adipocytes and skeletal muscles. Results in **adiponectin**, cytokine secreted by fat tissue increasing # of insulin-responsive adipocytes and regulates FA oxidation

**Thiazolidinediones** (pio**_glitazone_)**

What Type II Diabetes drug **decreases the enzyme activity of disaccharidases in intestinal brush border = decreased absorption of carbs** and reduced post-prandial hyperglycemia?

Alpha-glucosidase inhibitors (**acarbose, miglitol**)

What Type II Diabetes drug is **a noncompetitive inhibitor of mitochondrial glycerol-3-phosphate dehydrogenase** = **significant reduction in hepatic glucose production.**

Metformin

What Type II Diabetes drug **increases insulin release from the pancreatic Beta cells?**

**Sulfonylureas**

First-line treatment for Wilson's Disease (copper accumulation in tissues and hepatic tissue damage)... 2 Copper Chelators?

D-penicillamine and Trientine

**VEGF Inhibitors**

Bevaci**zumab** and Ranibi**zumab**

\_\_\_\_\_\_\_\_\_\_: **a somatostatin analog** used to control symptoms of **carcinoid syndrome.** Symptoms: flushing, watery diarrhea, bronchospasm, dyspnea, wheezing also used to inhibit secretory diarrhea in VIPomas (pancreatic endocrine tumors)

Octreotide

\_\_\_\_\_\_\_\_\_: **a dopamine agonist** used in growth hormone-secreting pituitary tumors or prolactinoma

Cabergoline

\_\_\_\_\_\_\_\_\_\_\_\_\_: a synthetic analog of GnRH. Continuous administration suppresses release of LH and FSH. -used in mgmt of prostate cancer, precocious puberty and endometriosis

Leuprolide

Phenoxybenzamine is an alpha blocker used to treat \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_.

Pheochromocytoma

\_\_\_\_\_\_\_\_\_\_\_\_\_\_ is a CD20 monoclonal antibody used to treat multiple myeloma, leukemia and multiple autoimmune disorders

**High-dose prednisone (corticosteroids) result in what changes in the CBC Differential (increase/decrease)?** Neutrophils Monocytes Lymphocytes Eosinophils Basophils

**INCREASED neutrophils** all others decreased to suppress immune system response and inflammation

Tx for CMV retinitis in an HIV patient?

Ganciclovir = against CMV DNA polymerase

Tx for Pneumocystis pneumonia

Pentamidine

\_\_\_\_\_\_\_\_\_\_\_\_\_\_: converted by fungal cytosine deaminase to 5-fluorouracil --\> RNA miscoding and inhibition of DNA synthesis. Used in combination with Amphotericin B for Cryptococcal infections.

Flucytosine

Treats Herpes simplex infections

Acyclovir

What drug should a newborn infant receive if they have congential hypothyroidism?

Levothyroxine (T₄)

**a partial opioid receptor agonist** that binds with high affinity (potency) to opioid mu-receptors but has low intrinsic activity (efficacy). **can displace other opioids and precipitate withdrawal** withdrawal: N/V, myalgias, dilated pupils, diaphoresis, tachycardia

Buprenorphine

NE leak causes intense alpha₁ receptor mediated vasoconstriction = leads to local tissue necrosis Antidote is a local injection in to the affected tissue with an **alpha₁ blocking drug**, such as _____________ resulting in vasodilation.

phentolamine

\_\_\_\_\_\_\_\_\_\_\_ can **mediate vasodilation via B₂ receptor activation**, particularly in **striated muscle, renal and mesenteric vascular beds**, leading to **decreased peripheral vascular resistance** with **increased cardiac output**

Isoproterenol

Antifungal drug? **binds microtubules** and **inhibits mitosis** \*ONLY tx **dermatophyte** fungi bc it accumulates in keratin-containing tissues

Griseofulvin

Antifungal drug? **inhibits DNA & RNA synthesis** \***Cryptococcal meningitis** with Amp B

Flucytosine

Antifungal drug? i**nhibits synthesis of polysaccharide glucan**, an essential component of the fungal **cell wall** \*Candida and Aspergillus

Echinocandins (**Caspofungin**, micafungin)

Antifungal Drug? **binds ergosterol in the cell membrane** leads to pore formation and cell lysis

**Amphotericin B and Nystatin** **\*Nystatin: oral candiasis (Swish and swallow)**

Antifungal drug? -**inhibits synthesis of ergosterol** (**cell membrane**)

Azoles

antifungal drug? - **accumulates in the skin and nails** - Tx **Dermatophytosis** **inhibits the fungal enzyme squalene epoxidase** = decreased ergosterol synthesis

**Terbinafine**

For Class I Antiarrhythmics, sodium channel binding strength is what order? What class has most use dependence d/t slow dissociation? What class has least use dependent d/t fast dissociation?

**IC \> IA \> IB** **Slow** Dissociation: **IC** (Flecainide, Propafenone) **Fast** Dissociation: **1B** (Lidocaine, Mexiletine) **1A**: Quinidine, Procainamide, Disopyramide

Best Class I Antiarrhythmic for **Ischemia-induced ventricular arrhythmias?**

**Class IB (Lidocaine, Mexiletine)** bc there is minimal cumulative effect over multiple cardiac cycles. (quick dissociation)

Treatment of Choice for **Listeria Meningitis?** ## Footnote **-has altered Penicillin-binding proteins (PBPs)**

Ampicillin \*not sensitive to cephalosporins

**First-line therapy** for **Streptococcus Pneumoniae Meningitis** (most common cause in **children \> 4 weeks old**)

3rd generation Cephalosporins (Cefotaxime, Ceftriaxone)

- **binds bile acids in the GI tract** - this **inhibits the enterohepatic circulation of bile acids** - diverts hepatic cholesterol to synthesis of bile acids, increased LDL cholesterol uptake from circulation and reduces LDL blood levels * *S/E**: **GI upset** and **impaired absorption of nutrients and drugs** * *Hypertriglyceridemia** (increases hepatic production of TGs)

**Bile acid-binding resins** (Cholestryramine, Colestipol, Colesevelam)

What class of drugs? - **decreases synthesis and increasing clearance of VLDL particles** - modest **reduction in triglycerides** - **inhibits HMG-CoA reductase**

Statins

- **inhibits the intestinal absorption of cholesterol** - **lowers LDL levels**

Ezetimibe

What class of drugs? - inhibit haptic production of TGs - FIRST LINE Tx for hypertriglyceridemia

Fibrates (Gemfibrozil, Fenofibrate)

What drug? - reduces blood triglyceride levels - raises HDL - decreases VLDL --\> LDL = decreased LDL concentrations

Niacin

What class of diuretics **increase Ca²⁺ reabsorption from the nephron** while **inhibiting the Na+/Cl- cotransporter in the distal convoluted tubule?**

Thiazides (Hydrochlorothiazide)

**Both Heparin and LMW Heparin** (negatively charged chemical naturally present in mast cells) **increase the effect of the naturally occuring anticoagulant** _______________ **by binding to it.**

Antithrombin III

\_\_\_\_\_\_\_\_\_\_\_\_\_: a **nondihydropyridine calcium channel blocker that acts by blocking L-type calcium channels**, preventing the initial calcium influx into cardiac myocytes and vascular smooth muscle cells. DOES NOT AFFECT SKELETAL MUSCLE CONTRACTILITY (b/c mechanical coupling occurs between L-type channels and RyR1)

Verapamil

antifungal - drug of choice for oropharyngeal candidiases without advance immunodeficiency - binds to ergosterol in the fungal cell membrane "swish and swallow" agent used commonly for asthmatics

Nystatin

a B1 and B2 adrenergic receptor agonist - increases myocardial contractility (B1) - decreased systemic vascular resistance aka vasodiation of peripheral vascular smooth muscle (B2)

isoproterenol

a sympathomimetic drug pure alpha adrenergic agonist vasoconstriction = inc SVR

Phenylephrine

acts on alpha-1 receptors = vasoconstriction = inc SVR -weak agonst at B1 receptors = modest inc myocardial contractility

Norephinephrine

selective B1 adrenergic blocking agent decrease contractility, HR and conductance

Esmolol

stimulates alpha-2 adrenoceptors in the brainstem = reduced sympathetic outflow from CNS - decrease in TPR, HR and BP - no effects on contractility

Clonidine

Binds to M₂ muscarinic receptors in the heart (dec HR and conduction velocity) also binds M₃ muscarinic receptors in the vasculature (vasodilation)

Acetylcholine

this **drug reduces the conversion of levodopa --\> dopamine** and consequently **minimizes systemic side effects** (N/V)

Carbidopa (a decarboxylase inhibitor)

what class of drugs **can be used to assist in the prevention of cerebral vascular spasm following a subarachnoid hemorrhage**?

Calcium Channel Blockers - **Nimodipine (cerebral selective drug)**

What inhaled anesthetic is known for causing hepatotoxicity and is metabolized extensibly by the liver?

Halothane

**a combination of extended-spectrum penicillin with B-lactamase inhibitor** effective **against most gram negative enteric rods** (**Pseudomonas**) and **anaerobic bacteria (Bacteroides** fragilis) including gram-positives

Piperacillin-Tazobactam

Tazobactam, Clavulanic acid and Sulbactam are all.... ?

B-lactamase inhibitors

antimicrobial that inhibits the synthesis of peptidoglycan, main component of **gram + bacteria** ## Footnote **covers MRSA and Clostridium Difficile**

Vancomycin

second-generation quinolone that acts by **interfering with bacterial DNA gyrase (topoisomerase II)**

Ciprofloxacin

a 3rd generation cephalosporin with poor anaerobic activity. activity against H. Influenzae, Klebsiella pneumoniae, Neisseria and Serratia

Ceftriaxone

a **selective peripheral dopamine-1 receptor agonist** - given IV to **lower blood pressure** in **Hypertensive emergency**, **especially beneficial for patients with acute renal injury (high creatine)** - **arteriolar dilation**, **inc renal perfusion** and **promotes diuresis and natriuresis**

Fenoldopam

\_\_\_\_\_\_\_\_\_\_\_\_\_\_: primarily used to reduce myocardial oxygen demain in acute coronary syndrome - rapid-acting venodilator - dec preload and CO

Nitroglycerin

- **alpha-adrenergic agonist** that causes an increase in systemic vascular resistance due to **arterial vasoconstriction** - **patients with hypotension or shock**

Phenylephrine

**2nd-line agent for treating acute gouty arthritis** **-for pts with contraindications to NSAIDS (peptic ulcer disease)** - **inhibits tubulin polymerization and microtubule formation** in leukocytes, **reducing neutrophil chemotaxis and emigration** to sites inflamed by deposition of crystals - **GI mucosal function impaired too --\> DIARRHEA\***, and some N/V and abdominal pain

Colchicine

a **highly sedating antidepressant** used to **treat insomnia** associated with depression S/E: **Priapism**

Trazodone

**Antiobiotic of Choice?** **Listeria monocytogenes** is a facultative intracellular, **gram-positive rod with distinctive flagellar-based tumbling motility seen at room temp.** - **multiply in cold temps** = grows well in refrigerated foods - transmitted transplacentally or via vaginal delivery = **neonatal meningitis**

**Ampicillin**

**short-acting selective B₂ adrenergic agonist** - **1st line treatment** for **acute bronchial asthma** - **bronchodilatory** effects

Albuterol

**anticholinergic agent** - **blocks action of ACh at muscarinic receptors** preventing bronchoconstriction = **bronchodilation** - **reduces parasympathetic stimulation (vagal)** of tracheobronchial submucosal glands in the lungs - COPD and asthma patients

Ipratropium

First-line Tx for PTSD includes trauma-focused cognitive behavioral therapy and ______________ (what class of drugs)?

antidepressant meds: SSRIs (and SNRIs also commonly used)

**Prokaryotic topoisomerase II (DNA gyrase)** is **inhibited by** ____________ antibiotics.

Fluoroquinolone

**Eukaryotic topoisomerase II (DNA gyrase)** is **inhibited by** the **anticancer drug** \_\_\_\_\_\_\_\_\_.

etoposide

**Acute treatment of agitation and psychosis** associated with **delirium** (changes in cognition and behavior) "confusional state" resulting in disorientation, agitation, psychosis and sleep distrubances typically d/t underlying medical condition (i.e. UTI in elderly)

**Low-dose 1st generation antipsychotics** (i.e. **HALOPERIDOL**)

an **intravenous osmotic diuretic** used primarily to **lower intracranial pressure (ICP)** and treat **acute glaucoma**

Mannitol

What **class of diuretics IMPROVES SURVIVAL** in patients with **congestive heart failure and reduced left ventricular ejection fraction?** -not to be used in hyperkalemic or renal failure pts S/E: Hyperkalemia and **Gynecomastia**

**Mineralocorticoid receptor antagonists** \*\***Spironolactone**, **Eplerenone**

What **class of diuretics** is frequently used for treatment of pulmonary congestion and fluid retention in heart failure patients? **Improves symptoms** significantly, but **DOES NOT provide survival benefit.**

Loop Diuretics - Fureosemide

What effects do simvastatin and cholestyramine have on hepatic cholesterol synthesis? effects on plasma LDL levels?

**Simvastatin:** **decreases cholesterol** synthesis by blocking HMG-CoA reductase **Cholestyramine**: **increases hepatic choleterol** synthesis d/t increased bile acid excretion **Synergistically: greater reduction in plasma LDL levels**

**Second-generation antipsychotics** that have lower risk of extrapyramidal side effects BUT **METABOLIC adverse effects** (**weight gain**, **dyslipidemia**, **hyperglycemia**, **increased risk of diabetes**) \*requires regular monitoring of fasting glucose and lipid profiles, blood pressures

Olanzapine

**Second-generation antipsychotic** with the potential life-threatening **side effect of AGRANULOCYTOSIS**

Clozapine

**Non-cardioselective beta blocker** can **trigger bronchospasm** and should be **avoided in patients with asthma or COPD.**

Propanolol Nadolol

**Cardioselective Beta Blockers with predominant B₁** receptor action are **safe in pts** with stable obstructive lung disease (**COPD, asthma)**.

**Metoprolol, Atenolol**, Bisoprolol, Nebivolol

What drug? **inhibits mycolic acid synthesis** **Mycobacterial TB resistance** through **non-expression of the catalase-peroxide enzyme** or through **genetic modification of the drug binding site** on the mycolic acid synthesis enzyme.

Isoniazid (INH)

inhibit synthesis of the mycobacterial cell wall

Ethambutol

Resistance to this drug in M Tuberculosis is primarily d/t a mutation in the gene that codes for a DNA-dependent RNA polymerase necessary for transcription and RNA prolongation

Rifampin

An aminoglycoside that inhibits mycobacterial protein synthesis by disabling the bacterial ribosomal 30S subunit (disrupting translation)

Streptomycin

The **antibiotic** ___________ **acts as an agonist at motilin receptors in the stomach and duodenum**, contributing to its **GI side effects.**

Erythromycin

VIP is secreted from pancreatic islet cells and increases loss of sodium, potassium, chloride and water in the stool = **secretory/watery diarrhea.** ## Footnote **VIP also inhibits gastric acid secretion.** **What drug inhibits the secretion of VIP?**

Somatostatin (Octreotide)

What **class of drugs are serotonin 5-HT_1B/5-HT_1D agonists** used as **abortive therapy during an acute migrane**?

**Triptans** (Sumatriptan)

\_\_\_\_\_\_\_\_\_\_\_\_\_: **monoclonal antibody** used in the mgmt of patients with **HER2-positive breast cancer** binds to portion of extracellular domain of HER2 receptor and **prevents activation of a transmembrane tyrosine kinase**

Trastuzumab

Tx for **premenopausal** pts with **ER-positive breast cancer.**

**Selective estrogen receptor modulators** (**Tamoxifen**)

Tx for **postmenopausal** women with **ER and/or PR overexpression breast cancer.**

**Aromatase inhibitors** (**anastrozole**, **letrozole**)

Human monoclonal Antibody against RANKL, used in bone metastatsis

Denosumab

Monoclonal antibody that act as VEGF inhibitors

Bevacizumab

Both maternal and fetal **cortisol help to accelerate lung maturation** **by stimulating surfactant production.** \_\_\_\_\_\_\_\_\_\_\_\_ or _____________ is **administered to pregnant women at risk of premature delivery to prevent respiratory distress syndrome.**

Beta**methasone** or Dexa**methasone**

name the class of drug that Pra**zosin** belongs to?

peripheral **alpha1-selective adrenergic blockers = vasodilation and reflex tachycardia**

What class of drugs f**orm free radicals in the myocardium and result in dilated cardiomyopathy** (biventricular CHF)?

**Anthracycline chemotherapeutic** **drugs** (doxo**rubicin**, dauno**rubicin**)

What is the **most effective method of preventing docorubicin cardiomyopathy**?

Dexrazoxane