Pharmacology Flashcards
Which immunosupresants agents cause nephrotoxicity? Which is their mechanism of action?
- Cyclosporine, Tacrolimus
- Calcineurin inhibitors – prevents IL-2 transcription
Why the PT and INR remain normal after two days of initiate warfarin?
Long half-life of factor II (prothrombin)
what is the reason to avoid antiacids (calcium carbonate) when use fluoroquinolones and tetracyclines?
Can chelate and decreased effectiveness of other drugs
which are the praziquantel and albendazol mechanisms of action?
- Praziquantel: increases the permeability of the membranes for calcium ions—induces contraction of the parasites, resulting in paralysis.
- Albendazol: inhibiting its polymerization or assembly into microtubules, decreased production por ATP.
why desmopressin is the treatment of von Willebrand disease?
Increases vWf release form weibel palade bodies from endothelial cells
- Drugs with low solubility in blood =
- Drugs with high solubility in lipids =
Give an example
- = Rapid induction and recovery times.
- = high potency = 1 /MAC
Examples: nitrous oxide (N2O) has LOW blood and lipid solubility, and thus fast induction and low
potency.
Halothane, in contrast, has high lipid and blood solubility, and thus high potency and slow
induction.
what is Imatinib?
Is tyrosine kinase inhibitor of BCR-ABL (Philadelphia chromosome fusion gene in CML) and c-kit
(common in GI stromal tumors).
which is the use of probenecid in neurosyphilis and gonorrhea?
in penicillin resistance cases, because increase the serum concentraction, inhibits organic anion transporters in kidney (penicillin are secreted by this transporters)
Clinical manifestations of hyperestrogenemia in cirrhotic patients
- Spider angiomata
- testicular atrophy
- dupuytren contracture
- Ginecomastia
- palmar erythema
- decreased body hair
Which is the reason to use paclitaxel in percutaneous coronary intervention?
paclitaxel binding to b-tubulin and prevents breakdown microtubules—- prevents stent restenosis by preventing intimal hyperplasia
Entacapone
Inhibit COMT (cathecol O- methyl transferase): increase bioavailability of levodopa by inhibiting peripheral inhibition
Bumetanide
Loop diuretic
Chlorlthalidone
thiazide diuretics: inhibit Na/ Cl cotransporter in distal convoluted tubule
Adverse effects: Hipokalemia, Hyponatremia, descreased insuline secretion and cause hypercholesterolemia
6- mercaptopurine
Is a cytotoxic purine analog— inhibits the novo synthesis of purines
Inhibited xantine oxidase
Do not give with allopurinol because increased toxicity or decreased effects
Calcipotriene
Psoriasis
Vit D analog: bind to the receptor and activated a nuclear transcription factor———- that inhibits keratiocyte proliferation
repaglinide
Meglitinides: secretagogous, insulin secretion— by clousing K+ channels
Foscarnet
pyrophosphate analog
used in CMV resistant to ganciclovir
could chelate calcium— hypocalcemia
Induced renal wasting of Mg —– Hypomagnesemia
Most common side effect of SSRI´s
sexual dysfunction
Most common side effectt of ethambutol
blurred vision secondary to optic neuropathy
blood/ gas partition
Anesthesic solubility in blood
If it is high= slower onset of action
Why nondyhidropyridine calcium channel blockers do not have effect in skeletal muscle?
Because skeletal muscle is not dependent on extracellular calcium influx
Varenicline
partial agonist of alpha4beta2 nicotinic acetyl choline receptor, competes with nicotine
Reducing nicotine craving
Hydroxyurea
Inhibits ribonucleotide reductase
increased fetal Hb synthesis
Fibrates and gallstones
Inhibit 7 alpha hydroxylase — catalyzes bile acids synthesis
Omalizumab
Anti IgG1 monoclonal antibody— binds to IgE inhibit the action
useful in severe asthma
Atropine poisoning
Anticholinergic syndrome, Hot, dry, red, blind and mad
antidote: physostigmine
Clordiazepoxide
long acting benzodiazepines with active metabolites—- as diazepam. Treatment in alcohol withdrawal
Finasteride
5alpha reductase inhibitor
conversion of testosterone to dihydrotestosterone
Treatment of BPH
fibrates
activating peroxisome proliferator activated receptor alpha (PPAR-alpha) —– increased synthesis of lipoprotein lipase
Thiazides diuretics
inhibits Na/Cl cotransporter in distal convoluted tubule —- decreasing reabsorption of Na and Cl—–decreased intravascular volumen– activating RAA system— increasing aldosterone—- increased K and H+ excretion— hypokalemia and metabolic alkalosis
Dapsone
mechanism of action similar to sulfonamides
useful in lepra treatment and P. jiroveci prophylaxis
adverse effects: hemolysis in G6PD deficiency
glipizide vs glubiride and glimepiride
short acting low risk of hypoglycemia (best option of elderly people)
glubiride and glimepiride long ancting more risk of hypoglycemia
How digoxin slows vetricular rate?
increasing parasympathetic tone — inhibits Na/K ATPase pump
and enhaces efferent parasympathetic ganglionic transmission—– increased vagal tone
Andrigenic alopecia treatment
5 alpha reductase inibitors: finasteride
Interaction between nitrates and phosphodiesterase inhibitors
Cyclic GMP accumulation
the arteriovennous concentration gradient in anesthesics mean?
tissue solubility
Large AV concentration= high solubility0 slow onset of action
Treatment in cyanide poisoning
- sodium nitrite
- sodium thiosulfate
- Hydroxycobalamine
Non nucleoside reverse transcriptase inhibitor
efavirenz
Nevirapine
*** Do not require activation via intracellular phosphorilation
Cocaine
Inhibited reuptake of monoamines: sympathetic stimulation
Halothane hepatitis
halogenates inhalated anesthesics (sevofluorane, desflorane, isoflorane)—————metabolized by CYP 450 — Reactive intermediates that could cause direct hepatocellular damage
trimethropine - methrotexate and pyrimetamine
inhibited dihydrofolate reductase
Clozapine
in schizophrenia resistant cases and associated with suicidatility
adverse effects: agranulocytosis
Amatoxins
Mushrooms poisoning
Inhibit DNA Polymerase II—— Synthesized mRNA: apoptosis
Direct thrombin inhibitor
Argatroban, dabigatran, bivalirubin
Nitrates exert their action by…..
vasodilation of peripheral veins and arteries (predominantly venodiltation)
decreased left ventricular wall stress (decreased preload) —- decreased end dyastolic pressure
decreased o2 demand of myocardial
adverse effects of thiazide diuretics
hypercalcemia----- decreased PTH hyponatremia Hypok Hypercholesterolemia Hyperglycemia hyperuricemia
Phencyclidine intoxication
PCP —- hallucinogen, combative behavior, nystagmus, ataxia
Antagonist of NMDA receptor ——- excess release of excitatory neurotransmitters
MAO inhibitors
phenelzine
tranylcypromine
Selegiline
Which is the reason to avoid MAO inhibitors and SSRI´s
increased the risk of serotonine syndrome
Colchicine
inhibits microtubules polymerization and leukotriene B4 synthesis
Selective estrogen receptor modulators
tamoxifen: adjuvant therapy in breast cancer
raloxifen: postmenopausal osteoporosis
Competitive inhibitor of estrogen binding (agonist or antagonist activity)
adverse effects: hot flashes, endometrial hyperplasia (tamoxifen only) and thromboembolism
neuraminidase inhibitors
inhibit viral particle release
Oseltamivir
Jimson weed
it is a plant: anticholinergic toxins
Cisplatin main adverse effect
ototoxicity: damaged stereocilia of hairy cells
which are the changes in HR and SBP with nitrates?
HR: increase— reflex tachycardia
BP: decrease— main venodilation
Pilocarpine
Contract ciliary muscle of eye
Cholicomimetic
Glaucoma and sjogren sx
Which is the effect of leuprolide in prostate cancer?
- is a GnRh analog
- continuous GnRH effect for long term leuprolide use—– supresses LH release ————– reduced production of testosterone. (similar effect of surgical orchiedectomy)
Anti TNF allpha agents
Infliximab: monoclonal antibody to TNF alpha
Etanercept: recombinant TNF receptor fusion protein
Aspirin
NON selective irreversible inhibiting COX-1 (and COX-2) —- inhibited the synthesis of TXA2 (potent stimulator of platelet aggregation)
Ehylene glycol poisoning
High aniongap metabolic acidosis
flank pain, gross hematuria and oliguria
calcium oxalate crystals
Drugs that are implicated in SLE drug induced
- procainamide
- hydralazine
- isoniazide
- minocycline
- TNF-Alplha inhibitors (etanercept)
Side effects of non dihydropyridine calcium channel blockers
dyltiazem and verapamil
constipation and AV block
methimazole and propylthiouracile
inhibit thyroid peroxidase (iodine organification and coupling of iodotyrosines)
propylthiouracile also decreaseperipehral conversion T4 to active T3
Norepinephrine
adrenergic agonist
alpha1: increased blood pressure (IP3 pathway) *** baroreceptor reflex (bradicardia)
and beta1 recerptors: increase cAMP (Gs) increased cardiac contractility, increased heart rate
RESULT: heart unchanged
Erythropoiesis stimulating agents adverse effects:
increase risk fir thrombosis embolic events— increase blood viscosity
Also develop hypertension (activation of erythropoietin receptors on vascular endothelium and smooth muscle cells
Ramelteon
melatonin agonist— suprachiasmatic nucleus (useful in insomnia en erderly patients)
Inhalation anesthesics
Increased GABA, Potassium channels (hyperpolarization of neuronal membranes), nicotinic and glycine receptors
- Myocardial depression
- Lungs: except nitrous oxide are respiratory depressants, decrease tidal volume and minute ventilation (hypercapnia), suppresion of mucociliar clearance (athelectasis)
- Brain: decrease vascular resistance — increase cerebral blood flow
- kidney: decrase glomerural filtration rate
- liver: decrease hepatic blood flow
Which is the reason of hemin and glucosa treatment in acute intermitent porphyria?
Down reagulating ALA synthase
becasuse the attacks in AIP are because the acummulation of ALA and PBG
succinylcholine adverse effects
hyperkalemia, hypercalcemia and malignant hyperthermia
Cell cycle independent drugs
- Cross. link DNA: interfere with replication
- alkylating agents: nitrosoureas, cyclophosphamide, busulfan
- platinum agents: cisplatin
Oxybutinin/tolterodine vs bethanecol
- antagonist of muscarinic receptor (urinary urgency)
2. Agonist of muscarinic receptor (pop ileus and urinary retention)
Renal ischemia with NSAIDS
PGS normally vasodilate the afferent renal arteriole
NSAIDS inhibits synthesis of PGS———– vasoconstriction of afferent arteriole
Bile acid binding resins
Cholestyramine, colestipol and colesevelam
Binding bile acids in Gi tract ———-inhibiting enterohepatic circulation ——————-decrease LDL levels, uptake of LDL.
Side effects: impaired absortion in gut and increase hepatic production of TAG———–Hypertryglyceridemia
Low distribution volume
3-5 L—— means high charged, the drug remains in the plasma
Relation between antihyoertensive drugs and K
** Thiazide and ACE inhibitors
Thiazide: HypoK
ACE inhibitors: HyperK
inhibitation Cox 1 and 2
COX 1: acetylation inhibits generation of TMX A2 in platelets
Cox 2: acetylation bloxks PGS production in inflammatory cells
Two specific symptoms of opiod withdrawal
Yawning and lacrimation
Nitrates and nitrites action mechanism
activate guanylyl cyclase— increased cGMP — myosin light chain dephosphorylation: relaxation
Imatinib
tyrosine kinase inhibitor of BCR-ABL—- useful in Chronic myeloid leukemia
lithium side effects
hypothyroidism
Nephrogenic diabetes insipidus
movements (tremor)
ebstein anomaly (cardiac, tricuspid valve)
Ribavirin
treat for hep C and respiratory syncytial virus
inhibited the synthesis of nucleotides: competitively inhibited inosine monophosphate dehydrogenase —- interferes duplicate of viral genetic material
Thiazolinedione
Pioglitazone and Rosiglitazone
Binds to PPAR-y nuclear transcription regulator (Decrease insuline resistance)
Side effect: Na reabsorption (be careful in heart failure)
Reed sternberg cells
distinctive tumor giant cells seen in Hodgkin lymphoma
Binucleated, bilobed (mirror images)
