click below
click below
Normal Size Small Size show me how
Pharmacology
UWORLD Pharmacology review
Question | Answer |
---|---|
Lidocaine is a class _____ antiarrhythmic that binds to ______________ channels and _____________________________. | IB; inactivated Sodium (Na+); rapidly dissociates |
Lidocaine and other IB antiarrhythmics are used for: | Treatment of ventricular arrhythmias induced by rapidly depolarizing and ischemic myocardium |
Adenosine is used to treat: | PSVT |
MoA of Adenosine: | causes transient conduction delay though AV node |
What is the mode of action of Digoxin: | 1. Enhanced vagal tone --> increased effective refractory period 2. Decreased conduction velocity through AV node |
Digoxin is used to treat: | Supraventricular arrhythmias (SVT) |
Dialtemzam is a class _____ antiarrhythmic. | IV |
What si the mode of action of Diltiazem: | 1. Slow sinus rate 2. Prolongs conduction through AV node 3. Decreased myocardial contractility |
What is the MoA of Diltiazem? | Used as rate-control agent for management of atrial arrhythmias (afib and aflutter) |
What are the 3 common Class IA antiarrhythmics? | Procainamide, Disopyramide and Quinidine. |
Class IA antiarrhythmics: | Bind to Na+ channels in the OPEN state and more specific for suppressing arrhythmias arising from areas of normal autonomacity. |
What other ionic effect is present in Class IA antiarrhythmics besides sodium blockage? | K+- channel blocking |
What is the MC treatment for HIT (Heparin-induced therapy)? | Direct Thrombin inhibitors (DTIs) |
What is the most common Direct thrombin inhibitor? | Argatroban |
Which anticoagulant is the MCC of thrombocytopenia in hospitalized patients? | Heparin |
HIT: | serious disorder caused by antibodies to heparin and platelet factor IV |
What are examples of Direct Thrombin Inhibitors (DITs)? | hirudin, Lepirudin, and Argatroban |
GP IIb/IIIa inhibitors: | inhibit binding GP IIb/IIIa with fibrinogen and fibronectin |
What are some common GP IIb/IIIa inhibitors? | Abciximab, Eptifibatide, and Tirofiban |
What is the MC use for GP IIb/IIIa inhibitors? | Percutaneous Intervention (PCI) in acute coronary syndrome |
Abciximab is an ________________________. | GP IIb/IIIa inhibitor |
What are two common SERMs? | Tamoxifen and Raloxifene |
Tamoxifen is an | selective estrogen receptor modulator |
Mode of action of Tamoxifen in breast cancer? | Competitive inhibitors of Estrogen binding to estrogen receptors |
What is an important side effect of Tamoxifen? | Estrogenic effect on uterus and can cause endometrial hyperplasia and cancer |
What are common adverse effects of SERM therapy? | 1. Hot flashes 2. Venous thromboembolism 3, Endometrial hyperplasia and cancer (Tamoxifen only) |
Raloxifene is used in post-menopausal women because? | It helps with Osteoporosis |
Tamoxifen can adversely develop: | Endometrial hyperplasia and/or cancer. |
Nucleoside analogue; Treatment of primary genital herpes | Acyclovir |
What is the mode of action of Acyclovir? | It incorporate, the nucleoside analogues, to the newly replicating viral DNA and ultimately terminate viral DNA chain synthesis |
Virus-encoded thymidine kinase? | Enzyme used by Acyclovir to convert acyclovir into acyclovir monophosphate. |
Cpss is? | steady-state plasma concentration |
WHat is the equation for maintenance dose? | Cpss x CL = ------------------ [Bioavailability fraction] |
What is the value of bioavailability in an IV drug? | 1 |
Loading dose = | Vd x Cpss = ----------------------- [bioavailability fraction] |
How is the loading dose altered in renal patients? | It remains unchanged |
Is Maintenance dose decreased or increased in Renal patients? | Decreased |
In a renal patient the loading dose _____________________, and the maintenance dose is _____________________. | Remains unchanged; Decreased |
What are the two main categories of anticonvulsants? | 1. Narrow Spectrum 2. Broad Spectrum |
What are the uses for Narrow Spectrum Anticonvulsants? | Treatment of simple and Complex seizures |
What are the Narrow spectrum anticonvulsants? | - Carbamazepine - Gabapentin - Phenobarbital - Phenytoin |
Carbamazepine, Gabapentin, Phenobarbital and Phenytoin are ________________________, wich are used to treat ___________ and ________ seizures. | Narrow Spectrum; Simple and Complex |
Which are the Broad spectrum anticonvulsants? | 1. Lamotrigine 2. Levetiracetam 3. Topiramate 4. Valproic acid |
For which kind of seizures are Broad spectrum anticonvulsants used for? | 1. Tonic-clonic seizure 2. Myoclonic |
What drug is used for Absence seizure? | Ethosuximide |
Ethosuximide is considered and _________--spectrum anticonvulsant. | Broad |
Lamotrigine, Levetiracetam, Topiramate, and Valproic acid are _________ spectrum anticonvulsants, used to treat _____________ and ___________ seizures | Broad; Tonic-clonic and Myoclonic seizures. |
Baclofen: | GABA-B agonist that can treat muscle spasticity, which is characterized by increased muscle tone and muscle spasms |
Example of a GABA - B agonist | Baclofen |
Fluphenazine: | dopamine antagonist that can treat Tourette syndrome |
What is a common drug to treat Tourette syndrome? | Fluzephine |
What is Tourette's syndrome? | Disorder characterised by motor or phonic tics that persists for more than 1 year. |
Benzodiazepine withdrawal? | Characterised by anxiete, tremor, insomnia, and sympathetic hyperactivity (diaphoresis, palpitation) |
What is a commonly used Benzodiazepine, that upon withdrawal commonly causes symptoms of withdrawal? | Lorazepam |
What are serious accompanying symptoms of Benzodiazepine withdrawal? | Psychosis, seizures,and death |
Opioid withdrawal? | characterized by nausea, vomiting, diarrhea, lacrimation l dilated pupils, and piloerection. |
Common aminoglycoside? | Gentamicin |
What is the most common way for acquiring resistance of aminoglycosides? | antibiotic-modifying enzymes |
What do the antibiotic-modifying enzymes do? | add chemical groups (methyl) to the antibiotic , which diminishes its ability to bid to the 16S ribosomal RNA (aminoglycosides) within the 30S ribosomal subunit. |
What is the most common origin of antibiotic-modifying enzymes? | Most arise via transfer of plasmids or transposons rather than chromosomal mutation. |
Vancomycin mode of resistance: | mutated peptidoglycan wall (D-ala-D-lac) |
Tetracyclines mode of resistance: | Impaired influx/ increased efflux |
Rifamycins mode of resistance: | mutated RNA polymerase |
Bisphosphonates include: | Alendronate and Risedronate |
What are some associated adverse effects of Bisphosphonate (Alendronate) therapy? | 1. Erosive (hemorrhagic) esophagitis 2. Increased risk of Osteonecrosis of the Jaw and, 3. Atypical femoral fractures + Hypocalcemia |
Osteonecrosis of the Jaw is often associated with the use of ___________________. | Bisphosphonates |
What is the drug of choice for Status epilepticus? | IV Lorazepam |
What is the MOA of Lorazepam? | Enhance the effect of GABA at the GABA-A receptor, leading to INCREASED CHLORIDE EFFLUX, and suppression of action potential firing. |
What receptor is blocked by Lorazepam? | GABA-A |
The blockage of the GABA-A receptor by Lorazepam leads to: | Increased Cl- efflux --> suppression of AP |
Benzodiazepine, such as Lorazepam, work on the _____________ membrane. | Post-synaptic |
What are the Presynaptic Ionic channels? | 1. Voltage-gated CALCIUM channel 2. Voltage-gated SODIUM channel |
What drug commonly blocks the Presynaptic Voltage-gated Calcium channels? | Gabapentin |
Phenytoin blocks the _______________-voltage-gated __________- channel. | Presynaptic voltage-gated Na+ channel. |
What are the 5 main receptors that cause vomiting? | 1. M1 (muscarinic) 2. D2 (dopaminergic) 3. H1 (histaminic) 4. 5-HT3 (serotonergic) 5. Neurokinin (NK1) |
What are the two vomiting receptors targeted in chemotherapy-induced vomiting? | 5-HT3 and NK1 receptors |
What drug is used to block the M1 receptor in treatment of vomiting? | Scopolamine |
For which condition is Scopolamine used for? | Motion sickness |
Which receptor is blocked by Scopolamine? | M1 muscarinic |
WHat are 3 antiemetic antihistamine drugs? | 1. Diphenhydramine 2. Meclizine 3. Promethazine |
What is the drug of choice of Promethazine? | Hyperemesis gravidarum |
Diphenhydramine and Meclizine are __________________, used in the treatment of ________________. | H1 antihistamines; emesis |
What are the 2 main D2 -receptor antagonist antiemetics? | Prochlorperazine and Metoclopramide |
Ondansetron and Granisetron are? | Serotonin (5-HT3) receptor antiemetics, used for Chemotherapy-induced emesis |
Serotonin antiemetics include? | Ondansetron and Granisetron |
NK-1 (neurokinin) receptor antagonists include? Used for? | 1. Aprepitant and Fosaprepitant Used for Chemotherapy induced emesis |
a-1 and a-2 adrenergic antagoisnt | Phenoxybenzamine |
Phenoxybenzamine: | irreversible a-1 & a-2 adrenergic antagonist that effectively reduces the arterial vasoconstriction induced by NE |
Phenoxybenzamine is considered an ________________________. | Non-competitive inhibitor |
Irreversible inhibitor is another way to name _________________. | Non-competitive inhibitor |
Non-competitive inhibitor effects ______________________- | Cannot be overcomed with increased concentration of drug due toe the binding to an allosteric site. |
What are common finding in Renal Artery Stenosis (RAS)? | Severe hypertension and Abdominal bruits |
RAS causes the activation of the __________ system. | RAAS |
Activation of the RAAS system causes: | 1. Increased RENIN secretion --> Increase in AT1 and AT2, which lead to an increased BP (blood pressure) 2. The increased BP leads to --> Increased Aldosterone secretion 3 Increased Aldosterone: - Increase renal Na+ reabsorption --> Relative Hypokalemia - Increase K+ and H+ secretion --> Metabolic alkalosis |
Activation of RAAS system is seen ultimately with: | Relative Hypokalemia and metabolic alkalosis |
Ganciclovir: | 1st line of treatment for CMV colitis and CMV-retinitis |
MOA of Ganciclovir? | Block CMV DNA polymerase |
SE of Ganciclovir: | Besides blockage of CMV-DNA pol, it can ALSO (lesser degree) block the Host's DNA polymerase, thus causing hematologic abnormalities. |
What are the hematologic abnormalities caused by adverse effect of Ganciclovir? | Neutropenia, anemia, and thrombocytopenia |
The fatigue and recurrent infection status of a patient with chronic treatment of CMV-colitis, may be due to what kind of drug interaction? | Ganciclovir indirect blockage of Host's DNA polymerase causing Neutropenia and anemia. |
What is the side effects seen with Vincristine? | Peripheral neuropathy and Neurotoxicity |
SE of Bleomycin | Pulmonary fibrosis and flagellate skin discoloration |
SE of Doxorubicin | Congestive heart failure |
SE of Cyclophosphamide | Hemorrhagic cystitis |
Daptomycin is used for: | Lipopeptide antibiotic with activity limited to gram positive organisms, including MRSA |
Daptomycin MOA: | 1. Depolarization of bacterial cellular membrane 2. Inhibition of DNA, RNA, and protein synthesis |
What are associated SE of Daptomycin? | 1. Increased creatine kinase (CK) 2. Increased incidence of Myopathy |
Phenylephrine is an ____________________________. | Selective a-1 receptor agonist |
What is caused or produced by Phenylephrine? | 1. Increase of Peripheral vascular resistance and Systolic PB 2. Decrease in Pulse pressure and Heart rate |
What are the low Potency (Non-neurological) 1st generation antipsychotics? | 1. Chlorpromazine 2. Thioridazine |
What are some side effects associated with Low Potency 1st generation antipsychotics? | - Sedation (histamine blockage) - Anticholinesterase -Orthostatic hypotension (a-1 blockade) |
Which drugs are considered High Potency (Neurological) 1st generation antipsychotics? | Haloperidol and Fluphenazine |
What are some SE associated with Haloperidol and Fluphenazine? | 1. EPS symptoms such as: - Acute dystonia - Akathisia - Parkinsonism |
MRSA is can be treated with ____________________. | Daptomycin |
Foscarnet is an: | analogue of PYROPHOSPHATE that can chelate Ca2+ and promote nephrotoxic renal Mg2+ wasting |
The __________________ and _______________- caused by _______________, may lead to development of ___________________. | Hypocalcemia and Hypomagnesemia; Foscarnet; Seizures |
What is the treatment for Serotonin Syndrome? | Cyproheptadine |
Bosentan is: | Competitive inhibitor of Endothelin receptors |
What is the Bosentan used for? | Treatment of Pulmonary Arterial hypertension (PAH) |
What are some NON-Benzodiazepine drugs? | Zolpidem, Zaleplon, Eszopiclone |
What is the MOA of nonbenzodiazepines? | Stimulate GABA-A receptors |
What is the clinical used of Zolpidem? | As a nonbenzodiazepine, used primarily hypnotics and don nor preuce the anxiolytic, muscle relaxant or anticonvulsants effects associated with benzodiazepines |
Why are non benzodiazepines used for treatment of insomnia and not the benzodiazepines? | Non-benzodiazepines DO NOT produce anxiolytic, muscles relaxant, or anticonvulsant effects. |
Ramelteon | Melatonin receptor agonist |
Suvorexant | Orexin receptor antagonist |
Cilostazol is a | phosphodiesterase inhibitor that inhibits platelet aggregation and acts as a direct arterial vasodilator. |
What is the common use for Cilostazol> | PAD (Peripheral arterial disease) |
What is the most common drug used for treating PAD? | Cilostazol |
Along with Cilostazol, the treatment of PAD is usually accompanied by: | Antiplatelet agent, such as Aspirin or Clopidogrel, for secondary prevention of coronary heart disease and stroke |
What is prevented by the addition of Aspirin to Cilostazol therapy for PAD? | SECONDARY prevention of coronary heart disease and stroke |
Cidofovir is: | Nucleoside monophosphate (nucleotide) that requires only cellular kinases for activation |
What are nucleotides? | Nucleosides with 1 or more attached phosphates |
What are common nucleotide drugs? | Cidofovir and Tenofovir |
Suffix used for "nucleotide" drugs? | -FOVIR |
Which are the acyclovir prodrugs? | Ganciclovir, Famciclovir, Valacyclovir |
What do Acyclovir and acyclovir prodrugs require for their activation? | Herpes Viral kinase and Cellular kinase |
What are two Cell-dependent Nucleosides? | Zidovudine and Lamivudine |
Activated Nucleotide analogue causes ----> | 1. Inhibition of DNA polymerase 2. Causes chain termination |
Aminoglycosides: | Inhibit genetic code and reading protein synthesis by dindin to the Prokaryotic 30S ribosomal subunit |
What are the associated adverse effects seen with Aminoglycosides? | 1. Ototoxicity --> Hearing loss and tinnitus (especially with loop diuretics) 2. Nephrotoxicity 3. Neuromuscular blockade 4. Teratogen |
The use of ____ a _________________ diuretic increases the risk of developing Ototoxicity if combined with __________, an _____________. | Furosemide -- Loop diuretic; Gentamicin -- Aminoglycoside |
Mode of Resistance of Aminoglycosides such as gentamicin? | Bacterial transferase enzymes (antibiotic-modifying) inactive the drug by acetylation, phosphorylation, or adenylation |
What is the clinical use for Aminoglycosides? | 1. Severe gram negative infections 2. Neomycin for Bowel surgery |
Sevelamer: | Non-absorbable anion-exchange resin that binds intestinal phosphate to reduce its absorption |
What is a common drug used in CKD patients in order to reduce phosphate levels? | Sevelamer |
What are the two kinds of Phosphate binders? | 1. Calcium-containing : calcium carbonate and acetate 2. Non-calcium contain: Sevelamer and Lanthanum |
Sevelamer and Lanthanum are: | Non-calcium containing phosphate binders. |
Benzodiazepines bind to the ________________ -site, which: | Benzodiazepine binding site; ALLOSTERICALLY modulates the binding to GABA, resulting in INCREASED frequency of Chloride ion channel opening |
Increased FREQUENCY of Cl- channel opening is caused by: | Benzodiazepines |
What causes he hyperpolarization and inhibition of action potential when using benzodiazepines? | The influx of Cl- into the neurons |
The increased Cl- influx to neuron causes: | 1. Neuronal hyperpolarization 2. Inhibition of Action Potential |
Valproic acid: | Reduce GABA catabolism |
Which drugs are examples of direct blockage of the lumen of ion channels? | Amiloride and Verapamil |
Amiloride: | affects the epithelial Na+ channels in the Distal portions of the nephron |
Verapamil | calcium channel bloker |
Verapamil and Amiloride are examples of: | Drugs that physically block the ion channel lumen |
Zidovudine is a | Cell-dependent nucleoside |
Nucleoside RT inhibitor example: | Zidovudine |
What drug is commonly used in HIV + mothers during labor in order to prevent HIV transmission? | Zidovudine |
Zidovudine features are: | Thymidine analogue that does not have a the normal 3-OH group found in thiamine |
The addition of nucleotides to the growing DNA chain is done by forming _________________________ at the 3'end. | Phosphodiester bonds |
The addition of Zidovudine to HIV therapy, works by: | Inability to form Phosphodiester bonds due to its abnormal 3-OH group. |
What is a specific side effect of Zidovudine? | Anemia |
What are common side effects of all NRTIs? | Bone marrow suppression and Peripheral neuropathy |
Bisphosphonates MoA: | chemical structure similar to PYROPHOSPHATE and attach to hydroxyapatite binding sites on bony surfaces to inhibit bone resorption by osteoclasts |
Bisphosphonates work on ____________________. | Osteoclasts |
Bisphosphonates prevent: | Bone resorption by osteoclasts |
Denosumab: | 1. binds to RANK-L and inhibits binding to RANK 2. Decrease differentiation and survival of Osteoclasts |
Recombinant PTH analogue example: | Teriparatide |
What is the MoA of Teriparatide? | - Stimulates maturation of Pro-Osteoblasts into bone forming osteoblasts - Increases GI calcium absorption and renal tubular Ca2+ reabsorption. |
What kind of drugs have a similar chemical structure to Pyrophosphate? | Bisphosphonates |
What are the main two Class IC antiarrhythmics? | Flecainide and Propafenone |
Flecainide is: | Potent sodium (Na+) channel blocker that have increased effect on faster heart rates |
SE: proarrhythmic effects | Class IC antiarrhythmics |
What is an example of an proarrhythmic side effect found in Class IC antiarrhythmics? | Prolongation of the QRS |
Class IC antiarrhythmics: | - Strong inhibition of Phase 0 depolarization - No changes in length of Action potential |
Class IB antiarrhythmics: | - Weak inhibition of Phase 0 depolarization - Shortened length of Action potential |
Class IA antiarrhythmics: | - Intermediate inhibition of Phase 0 depolarization - Prolonged length of action potential |
What class of antiarrhythmics that block sodium channels, produce a strong inhibition of Phase 0 depolarization? | Class IC |
Shortened length of AP is seen with: | Class IB antiarrhythmics |
Prolongation in length of action potential is common in _________ sodium channel blockers antiarrhythmics. | Class IA |
Opiate analgesics work by: | Reduce pain by binding to Mu receptors and inhibition synaptic activity in the CNS |
Opioids may work on the ________________ or _____________ cell membrane of neurons. | Presynaptic ; Postsynaptic |
What occurs in times that opioids work on Presynaptic mu receptors? | - Closedure of Voltage-gated Calcium channels and, - Decrease excitatory NT release |
At times that opioids bind to postsynaptic Mu receptors, it causes: | 1. Opening of K+ channels 2. Membrane Hyperpolarization |
Which mu receptors need to be activated by opioids in order to close the Voltage-gated Calcium channels? | Presynaptic Mu receptors |
Membrane hyperpolarization and K+ channel opening in a neuron after mu receptor activation is due: | Opioid binding to Postsynaptic Mu-receptors. |
Bleomycin MOA: | antineoplastic agent that binds to IRON and OXYGEN molecules to create FREE RADICALS that cause DNA strands to break. |
MC side effect of Bleomycin is: | Lung toxicity, which is presented by PULMONARY FIBROSIS |
Pulmonary fibrosis caused by Bleomycin is presented with: | Dyspnea and non-productive cough and PTFs show a Restrictive pattern with decreased diffusion capacity of Carbon monoxide (DLCO) |
MoA of Doxorubicin | 1. Binds to Topoisomerase II to cleave DNA 2. Binds to iron to generate free radicals |
SE associated with Doxorubicin | Dilated cardiomyopathy |
Example of an anthracycline: | Doxorubicin |
MoA of Cisplatin | Cross-links DNA to inhibit DNA synthesis |
SE associated with Cisplatin: | - Nephrotoxicity - Ototoxicity - Peripheral neuropathy |
Cyclophosphamide MoA: | Cross-links DNA to inhibit DNA synthesis |
What are the most common side effects of Cyclophosphamide therapy? | 1. Hemorrhagic cystitis 2. Bladder cancer |
What is the mode of action of Paclitaxel? | Inhibition of microtubule disassembly |
What is the mode of action of Vincristine/Vinblastine? | Binds to B-tubulin to inhibit microtubule formation |
What is the shared side effect seen with Paclitaxel and Vincristine/Vinblastine? | Peripheral neuropathy |
Inhibition of microtubule assembly is seen in ____________________, while inhibition of microtubule formation due to binding of B-tubulin is associated with __________________. | Paclitaxel; Vincristine/Vinblastine |
BCL-2 inhibitor is used to treat __________________. | CLL |
What is a common BCL-2 inhibitor? | Venetoclax |
Mode of action of BCL-2 inhibitor? | cause cancer cell death by promoting cytochrome c release form the mitochondria, which subsequently activates caspases. |
Rituximab: | antibody against B-cell marker CD20 |
Olaparib: | Inhibits poly-ADP ribose polymerase, the enzyme that repairs single-stranded DNA breaks |
Bortezomib: | Proteasome inhibitor that prevents destruction of Ubiquitinated intracellular proteins. |
Which organs have rapid drug distribution? | Brain, Liver, kidneys, lungs, and heart |
Why do the brain, liver, lungs, kidney, and heart have a rapid drug distribution? | Due to accelerated and/or rapid blood flow |
Which organs are depicted as poorly vascularized, thus with slow drug distribution? | Those with reduced blood flow such as Skeletal muscle, fat, and bone. |
Which type of drugs bind to antithrombin and increase the activity against factor Xa? | Unfractionated Heparin and LMWH |
What is the action of Unfractionated Heparin and LMWH? | bind to ANTITHROMBIN in order to increase its activity against Factor Xa |
What is a key feature of Unfractionated Heparin, not shared by LMWH? | Only Unfractionated heparin binds to both, ANTITHROMBIN and THROMBIN to allow antithrombin to inactivate thrombin |
Unfractionated Heparin binds to: | Antithrombin and Thrombin, both |
Unfractionated heparin binding to antithrombin and thrombin causes? | Antithrombin to inactivate thrombin. |
Common cardiac use of Atropine? | Bradycardia |
How is bradycardia treated by Atropine? | Decreases vagal influence of SA and AV nodes (increase HR) |
What is a common side effect of Atropine | Increase intraocular pressure |
Acute Closed-angle Glaucoma: | Presents with UNILATERAL eye pain and visual disturbances (Halos). |
What kind of individuals have higher risk of developing Closed-angle glaucoma when treated with Atropine? | Inuit and Asian descent |
Inhibit enterohepatic circulation of bile acids | Bile acid-binding resins |
What is a adverse effect of Bile acid resin monotherapy? | Increased hepatic production of TGs---> Hypertriglyceridemia. |
Bile acid resins cause: | 1. Diversion of hepatic cholesterol to synthesis of newl bile acids 2. Increase uptake of cholesterol from circulation 3. Reduced blood LDL levels |
What kind of drugs precipitate Neuroleptic Malignant Syndrome (NMS)? | Dopamine antagonist |
How is NMS similar in symptoms to Serotonin Syndrome? | BOTH present with altered mental status and sympathetic hyperactivity. |
What are the distinguishable features of NMS? | 1. Diffuse muscle rigidity 2. Hyporeflexia |
What is the common treatment for NSM? | Dantrolene and Benzodiazepines |
What is the precipitant for Serotonin Syndrome? | Serotonergic agent |
What are the distinguishing features of Serotonin syndrome? | Clonus and hyperreflexia |
Why does Buprenorphine causes precipitation of opioid withdrawal syndrome? | It has a partial agonist effect that causes the displacement of other opiates used concurrently |
Effects of competitive inhibition cause changes in: | Potency |
A left shift in drug curve graph, means? | Increase in Potency |
A up or down shift in a drug-curve graph, represents: | Change in Efficacy |
Changes in Efficacy have the same | Vmax |
A change in efficacy is accomplished by _____________________ inhibition, which a change in potency is done by ________________ inhibition. | Efficacy ----> Non-competitive Potency -----> Competitive |
The suffix "mab" represents: | Monoclonal antibody |
" -cept" represents: | Receptor molecule |
"-nib" suffix indicates: | Kinase inhibitor |
Etanercept: | Receptor molecule that acts as a decoy receptor. |
Etanercept is: | Fusion protein of TNF-a receptor to IgG1 |
What effects occur on WBC count with the chronic use of corticosteroids? | Increase Neutrophil count Decrease lymphocyte, monocyte, basophil, and eosinophil counts |
Why the increase levels of Neutrophils in patients on corticosteroids? | Due to the "demargination" of neutrophils previously attached to the vessel wall |
"Demargination" is associated with: | The increase levels of neutrophils seen in corticosteroid use |
Skin effects of corticosteroids; | 1. Central obesity, "buffalo" hump 2. Skin atrophy, bruisability (decreased collagen and fibroblast) 3. Proximal muscle weakness |
What are the endocrine effects on chronic use of corticosteroids? | - HPA axis suppression - Hyperglycemia -Hypogonadism - Osteoporosis (decreased bone formation , and decrease Ca/Phosphate absorption) |
What is the main immune effect of chronic use of corticosteroids? | Neutrophilia (neutrophil demargination) |
What some CNS effects seen in prolonged corticosteroid use? | Hypomania, Psychosis, and Sleep disturbance |
Prolonged use of corticosteroids may increase the ____________ production. | Surfactant |
What drugs contribute to long-term survival in patients with HF due to LV systolic dysfunction? | 1. B-blockers --> carvedilol, metoprolol 2. ACE inhibitors --> " -pril" 3. ARBs ----> Losartan 4. Aldosterone antagonists ---> Spironolactone, Eplerenone |
Which two kind of cardiac/renal medications have not proven any long-term survival benefits? | Calcium channel blockers and Diuretics (except for K+ sparing) |
Fenoldopam: | Selective Peripheral Dopamine-1 receptor agonist. |
Hypertensive emergency is considered with: | BP > 180/120 mm Hg + End-organ damage. |
What is a common drug given to CKD patient with a persistent BP of 200/120 mm Hg? | Fenoldopam |
What are the expected effects of Fenoldopam? | 1. Arteriolar dilation 2, Increases renal perfusion 3. Promotes diuresis and Natriuresis |
Why is Fenoldopam used in renal insufficiency patients? | It provides benefit to the kidney function by: - Increasing the renal perfusion and - Promoting diuresis and Natriuresis |
What is the difference between Hydralazine and Fenoldopam use in Hypertensive emergencies? | Fenoldopam is usually used in renal insufficiency patients, due to its effects on the kidneys, while Hydralazine doe not provide such benefits. |
What are the associated side effects of Hydralazine? | Reflex tachycardia and Sodium and fluid retention |
What is the 1st line of treatment for Trigeminal neuralgia? | Carbamazepine |
What is the MoA of Carbamazepine? | Inhibits neuronal high-frequency firing by reducing the ability of Na+ channels to recover form inactivation |
What are two common side effects of Carbamazepine? | 1. Bone marrow suppression 2. SIADH which leads to Hyponatremia |
Which drugs block the NMDA receptors? | Ketamine, Felbamate, and Memantine |
What is the common use of Memantine? | Treatment of Alzheimer dementia |
Felbamate is an _____________ blocker that is used an an ________________. | NMDA receptor blocker; Anticonvulsant |
Ketamine is used as an | general anesthetic |
What drug irreversibly blocks P2Y component of ADP receptors on the platelet surface and prevents platelet aggregation? | Clopidogrel |
What receptors are blocked by Clopidogrel? | P2Y |
What drugs are used to prevent Thrombotic events? | Apixaban( direct factor Xa inhibitor), and Warfarin |
Which kind of drugs are used in acute coronary syndrome? | LMWH |
Inhibition of platelet aggregation is done by? | Aspirin and Clopidogrel |
What is the mode of action of Metformin? | 1. Inhibits mitochondrial glycerophosphate dehydrogenase and complex I 2. Upregulates AMP-attached protein kinase |
What are the metabolic effects seen with Metformin? | 1. Decrease hepatic glucose production 2. Increase peripheral glucose uptake/ utilization |
What are some adverse effects seen with Metformin? | - Diarrhea - Lactic acidosis (increased risk of renal insufficiency) |
How is metformin excreted? | Renal clearance |
Oseltamivir is an: | Neuraminidase inhibitor |
What is a common antiviral used for Influenza A and B? | Oseltamivir |
What is the action of Oseltamivir? | Prevents newly formed virios for infected host cells and impairs viral penetration of mucous secretion that overlie the respiratory epithelium |
Amantadine | Impairs viral uncoating; used in Parkinson dementia |
What is a common antiviral used in Parkinson dementia? | Amantadine |
Amantadine is used to treat _______________________ ____________. | Parkinson dementia |
What is the most common cause of death due to overdose of TCA? | cardiac arrhythmias and refractory hypotension due to inhibition of Fast Na+ channel in cardiac myocytes. |
What are the clinical signs of inhibitory effects of muscarinic ACh receptors due to TCA overdose? | Tachycardia, delirium, dilated pupils, flushing, decreased sweating, hyperthermia, ileus, and urinary retention. |
What is PD-L1? | Ligand the bids to PD-1 on cytotoxic T-cells and inhibit their response. |
What is the relation between on PD-L1 and cancer cells? | Cancer cells avoid immune recognition by overexpressing PD-L1. |
What is the clinical features Hypokalemia? | Muscle weakness, cramps and possible rhabdomyolysis. |
What is caused by Thiazide diuretics? | Decrease of intravascular fluid volume which lead to Aldosterone production which case Increased K+ and H+ secretion in urine |
Relative Hypokalemia and metabolic alkalosis is common in the use of __________________________ diuretics. | Thiazide |