Pharm Flashcards
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)
Treatment for Arsenic poisoning (hypotension, garlic odor on breathe)
-insectisides, contaminated water
Dimercaprol (i.e. British Anti-Lewisite) increases urinary excretion of heavy metal
adverse reaction to antipsychotic meds (i.e. given during manic episodes)
Neuroleptic Malignant Syndrome (NMS) = hyperthermia (fever), msucle rigidity and confusion
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)
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
directed against the CD20 antigen (B-cell marker) and improves the prognosis of some lymphomas (i.e. non-hodgkin’s lymphoma)
Rituximab
a monoclonal antibody used in treatment of breast cancer
trastuzumab (Herceptin)
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
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
used to treat onchocerciasis (river blindness)
Ivermectin
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)
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
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
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)
What drugs can be used to control severe Graves’ ophthalmopathy?
-decreases severity of inflammation and decreases extraocular volume
High-dose Glucocorticoids (prednisone)
what 2 drugs inhibit thyroid peroxidase, thus reducing iodine organification?
Methimazole and Propylthiouracil
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
Name 3 antibiotics commonly used for invasive methicillin-resistance Staphylococcus Aureus infections.
- Vancomycin
- Daptomycin
- Linezolid
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
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
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
- 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
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
more selective aldosterone antagonist with fewer side effects
Eplerenone
Topical prostaglandin that increases outflow of aqueous humor via the uveoscleral pathway.
Preferred Tx for Open-Angle Glaucoma
Latanoprost
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 (propanolol)
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).
- Lamotrigine
- Levetiracetam
- Topiramate
- Valproic Acid
Name some Narrow Spectrum anti-convulsants used to treat Focal Epilepsy (Simple and Complex)
- Carbamazepine
- Gabepentin
- Phenobarbital
- 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
anthracyclines
Daunorubicin and Doxorubicin
________________ are first-line Tx for acute gouty arthritis. They inhibit cyclooxygenase decreasing PGs synthesis and exert a broad anti-inflammatory effect that includes inhibition of neutrophils.
NSAIDs (naproxen, indomethacin)
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)
(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)
gardening
Physostigmine (cholinesterase inhibitor)
First-line treatment for alcohol withdrawal?
If 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