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Rapid Review Step 1 > Pharma > Flashcards

Pharma Flashcards

1
Q

QT Prolongating Drugs

A

Class Ia antiarrhythmics (eg, quinidine)
Class III antiarrhythmics (eg, dofetilide, sotalol
Macrolides & fluoroquinolones
Antiemetics (eg, ondansetron)
Azoles (eg, fluconazole)
Antipsychotics, TCAs & SSRIs
Some opioids (eg, methadone, oxycodone)

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2
Q

Sulfonylureas
Meglitinides

A

Glubyride, Glipizide, Glimeperide, Chlorpropramide

Mechanism of action
↑ Insulin secretion by inhibiting β-cell K+ ATP channels and Ca+2 influx
S/E
Hypoglycemia
Weight gain

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3
Q

Biguanides

Metformin

A

Stimulate AMPK & inhibit mitochondrial gluconeogenesis, ↓ hepatic glucose production & ↑ peripheral glucose uptake, Increases insulin senstivity.
S/E
Diarrhea
Lactic acidosis

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4
Q

Thiazolidinediones

Pioglitazone

A

Activate transcription regulator PPAR-γ, ↓ insulin resistance
S/E
Fluid retention/heart failure
Weight gain

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5
Q

GLP-1 agonists

Exenatide
Liraglutide

A

↑ Glucose-dependent insulin secretion, ↓ glucagon secretion, delayed gastric emptying
S/E
Pancreatitis
Weight loss

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6
Q

DPP4 inhibitors

Sitagliptin
Saxagliptin

A

↑ Endogenous GLP-1 & GIP levels
S/E Nasopharyngitis

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7
Q

SGLT-2 inhibitors

Canagliflozin
Dapagliflozin

A

↑ Renal glucose excretion
S/E
Urinary tract infections
Hypotension

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8
Q

Selective estrogen receptor modulators (SERMs)

A

tamoxifen, raloxifene
MOA Competitive inhibitor of estrogen binding
Mixed agonist/antagonist action
S/E Hot flashes
Venous thromboembolism
Endometrial hyperplasia & carcinoma (tamoxifen only)
Uterine sarcoma (tamoxifen only)

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9
Q

Bisphosphonates

A

alendronate, risedronate
are used to treat osteoporosis and act by inhibiting osteoclast-mediated bone resorption.

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10
Q

Denosumab

A

Binds RANKL & inhibits binding to RANK
Reduces differentiation & survival of osteoclasts
Used in Osteoporosis

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11
Q

Recombinant PTH analog (Teriparatide)

A

(teriparatide)
Stimulates maturation of preosteoblasts into bone-forming osteoblasts
Increases gastrointestinal calcium absorption & renal tubular calcium reabsorption

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12
Q

Statins

A

HMG Co A Reductase Inhibitor , LDL receptor upregulation
Atorvastatin, Rosuvastatin, Simvastatin
Dec LDL
Inc HDL
Dec S.TG
Pravastatin is only statin that undegoes renal excretion

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13
Q

B-Blockers Overdose

A

Treat with Glucagon
Activates G-protien coupled receptors on cardiac myocytes causing activation of adenalyl cyclase & raising intracellular cAMP results in Ca+2 release and Increase SA node firing rate.

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14
Q

Bupropion

A

Inhibit reuptake of NE and dopamine.
Used to treat MDD(1st line)
No sexual side effects
increase dosage have high risk for siezure
C/I seizure disorder, bulemics and anorexia

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15
Q

Ramelteon

A

Melatonin agonist
used for insomnia in elderly, it has lowest side effects among all the sedatives.

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16
Q

Ipratropium

A

Muscarinic Antagonist
Competitively block muscarinic receptor to prevent bronchoconstriction
used in Asthma

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17
Q

Beclomethasone, Prednisone

A

Corticosteroids
Inhibit Leukotriene Synthesis
reduce inflammation leads to bronchodilation
used in COPD & Asthma
S/E: Osteoporosis, Cushingoid reaction, glucose intolerance, infection ,HTN, cataracts

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18
Q

Methylxanthines

A

Theophylline
Inhibits PDE > dec cAMP Hydrolysis (inc cAMP) promoting bronchodilation
Used for Asthma
S/E: Cardiotoxicity, Neurotoxicity

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19
Q

Cromolyn

A

Prevent release of mediators from mast cells
used in asthma prophylaxis

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20
Q

Zileuton , Zafrilukast, Montelukast

A

Anti-leukotrienes
5-lipoxygenase inhibitor > inhibit conversion of arachidonic acid to leukotrienes > prevents bronchoconstriction & inflammatory cell infiltrate
used for aspirin induced asthma

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21
Q

Diphenhydramine, Chlorpheniramine

A

1st gen H-1 blockers
reversible inhibitor of H-1 histamine receptor
used for allergy, motion sickness, sleep aid
S/E: Sedation, Antimuscarinic (Hot as Hare), anti alpha adrenergic (sudden drop in BP)

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22
Q

Guaifenesin

A

Expectorant
removes excess sputum but does not suppress cough reflex
Used for minor URI, Common cold w/cough

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23
Q

N-acetyl cysteine

A

Expectorant
loosens mucus plugs by breaking di sulfide bonds
used for Cystic fibrosis, antitode for Acetaminophen OD

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24
Q

Loratadine, Fexofenadine, Desloratadine, Cetirizine

A

2nd Gen H-1 blockers
less sedating than 1st gen cuz dec entry into CNS
Used for Allergy

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25
Q

Bosentan

A

Competitively antagonizes endothelium-1 receptors decreasing pulmonary vascular resistance
Used for Pulmonary HTN

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26
Q

Pseudoephedrine, Phenylephrine

A

Sympathomimetic alpha-agonists,
nasal decongestants
Pseudoephedrine is is alpha-1 specific
Reduces Hyperemesis. Edema, Nasal Congestion and opens obstructed Eustation tubules
S/E: HTN, CNs stimulation/Anxiety

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27
Q

Salmeterol

A

B-2 agonist : relaxes bronchial smooth muscles
Long Acting (LABA) used for prophylaxis of Asthma/COPD
S/E: Tremor & Arrhythmia

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28
Q

Albuterol

A

B-2 agonist : relaxes bronchial smooth muscles
Used for Acute exacerbation of Asthma

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29
Q

Isoproterenol

A

Non-specific Beta agonists, relaxes bronchial smooth muscles (B2)
Used for Bronchoconstriction due to sympathetic tone
S/E: Tachycardia

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30
Q

Methacholine

A

Muscarinic receptor Agonist
Used in asthma challenge test

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31
Q

Dextromethorphan

A

Anti tussive, Antagonizes NDMA & Glutamate Receptors
S/E: Mild Opioid effect so mild abuse potential

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32
Q

Desmopressin DDAVP

A

Mild hemophilia A & Type 1 von Willebrand disease:
Increases circulating factor VIII & endothelial secretion of vWF to stop bleeding.

Central diabetes insipidus & Nocturnal enuresis:
Binds to V2 receptors in renal tubular cells, leading to increased aquaporin channels, increased water reabsorption & decreased urine output

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33
Q

Fibrates

A

(Fenofibrate, Gemfibrozil)
Upregulates Lipoprotien Lipase
results in inc oxidation of FA
Inhibit cholesterol 7 alpha- hydroxylase
increase risk of cholesterol gallstones

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34
Q

Ursodiol

A

Decrease cholesterol secretion into bile thereby preventing the cholesterol gallstones formation
2nd line for cholelithiasis after cholecystectomy (1st line)

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35
Q

Heparin

A

Unfractioned Heparin, LMWH
Prevent Factor X->Xa
Antitode Protamine Sulphate
Can cause Heparin induces Thrombocytopenia

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36
Q

Warfarin

A

Vitamin-K antagonist of Vit-K dependant factors 2, 7, 9, 10, protien C & S.
Antitode Vit-K & Fresh Frozen Plasma (immideate reversal)

Originated as Rodenticide still found in most rat poisons and there exposure can serve as oxidizing agent for post-translational gamma carboxylation of glutamate residues and can lead to coagulopathy.

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37
Q

Factor Xa inhibitors

A

Inhibits factor X->Xa
Direct: Rivaroxaban, Apixaban
Indirect: parinaux

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38
Q

Agatroban, Bivalirudin

A

Direct thrombin Inhibitors
Inhibit prothrombin to thrombin conversion
II -> IIa inhibition

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39
Q

Clopidogrel

A

P2Y-12 receptor blocker/ platelet ADP receptor (P2Y-12) blocker.
Antiplatelet aggregation
Action similar to aspirin which is Thromboxane A2 inhibitor.
Used in patients with aspirin allergy as replacement for aspirin

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40
Q

HydroxyUrea

A

Inhibit Ribonucleotide Reductase
Decrease DNA synthesis
Used in Sickell cell anemia & CML
Increase HbF
S/E: long use causes Myelosuppression

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41
Q

Ruburicase/ Pioglitacase

A

Recombinant Uricase
Catalyses the metabolism of uric acid to allantoid which is more dissolveable, excretable and less toxic & less chance of precipitation than uric acid

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42
Q

Fludocortisone

A

Steroid acts as Aldosterone
Used in 21-hydroxylase deficiency and in patients with low aldosterone

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43
Q

Sevelamer

A

Non absorbable phospate binder that prevents phosphate absorbtion from GI tract

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44
Q

Methimazole

A

Blocks TPO
Prevents Iodination and Coupling
S/E: Teratogenic C/I in first trimester

Note:
Methimazole is preferred to PTU because PTU is Hepatotoxic, In pregnancy PTU is used instead of Methimazole due to teratogenicity of Methimazole (Aplasia cutis, Esophageal atresia, Facial anamolies) but after that patient is shifted back from PTU to Methimazole

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45
Q

PTU (Propiothiyouracil)

A

Blocks TPO
same as Methimazole unlike methimazole also blocks already active harmone methimazole only block production.
S/E: Agranulocytosis
Note:
Methimazole is preferred to PTU because PTU is Hepatotoxic, In pregnancy PTU is used instead of Methimazole due to teratogenicity of Methimazole (Aplasia cutis, Esophageal atresia, Facial anamolies) but after that patient is shifted back from PTU to Methimazole

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46
Q

Liothyroinine/ Levothyroxine

A

Liothyronine: T3
Levothyroxine: T4

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47
Q

Patiromer

A

Chelator in GI tract
S/E: Diarrhea, GI disturbance, Hypokalemia

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48
Q

Acarbose/ Miglitol

A

Antidiabetic
Inhibits intestinal brush border A-glucosidase
S/E: Diarrhea, Malabsorbtion (Blunting of GI brush borders)

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49
Q

Cinacalcet

A

Used for hypocalcemia due to CKD or PTH
Increases Ca+2 receptor senstivity, when it senses calcium provides feedback inhibtion to PTH.

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50
Q

Tolvaptan

A

ADH receptor antagonist (reversible)
Used to treat SIADH

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51
Q

Demclocycline

A

Tetracycline
Damages ADH receptor (irreversible)

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52
Q

Rifampin

A

Inhibits DNA dependant RNA polymerase
Used for TB (non-negotiable med)
S/E:
CYP inducer
Red/Orange secretions (i.e Urine)
Hepatotoxicity
Avoid with PTU which is also hepatotoxic

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53
Q

INH (Isoniazid)

A

Prevent Myocolic acid through activation of KAT-G mutation
Used for TB (non-negotiable med)
S/E:
Peripheral Neuropathy ( can be prevented by Vit-B6 supplementation)
Lupus rash
Hepatotoxicity

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54
Q

Pyrazinamide

A

Accumulation of pyrazonic acid, decrease proton motive force, decrease EN2F (X)
Used in TB (negotiable med)
S/E:
Hepatotoxic
Hyperurecemia
C/I in pregnancy

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55
Q

Ethambutol

A

Inhibits arabinosyl transferase (decrease cell wall production)
Used in TB (negotiable med)
S/E:
Optic neuritis
C/I in SLE

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56
Q

Mofetil, Mycophenolate

A

Affects purine pathway, IMP-dehydrogenase
S/E:
GI problems
Pancytopenia

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57
Q

Eculizumab

A

Monoclonal antibody affecting complement especially C-5

58
Q

Omalizumab

A

Monoclonal antibody
Prevents IgE binding to mast cells by blocking the receptor, prevents degranulation
Used in people with allergy

59
Q

Sucralfate

A

Attaches on top of ulcer provides physical protection and allows HCO3– to re-establish the PH gradient and allows healing.
S/E: Diarrhea

60
Q

Sulfasalazine

A

Combo of Antibacterial + Anti inflamatory
Salfapyridine + 5-aminosalicyclic acid (aspirin)
Requires activation by colonic bacteria
S/E:
Diarrhea > Malabsorbtion
Reversible Oligospermia

61
Q

Metoclopramide

A

D-2 antagonist
Also Antagonist of Serotonin 5HT3 & Agonist of 5HT4 receptors
Increase GI motility
Used in gastritis, ulcer, gastroparesis
S/E:
Diarrhea
Extrapyramidal SE ( Dystonia, Akathesia, Parkinsonian symptoms)

62
Q

Anti-parasympatheitics

A

Anti-Cholenergic , Anti-muscuranics
Atropine: Rx cholenergic poisoning, unstable bradycardia
Scopalamine: Tx Motion Sickness
Benztropine: Tx Extrapyramidal SE
Trihexphenidyl: Tx Extrapyramidal SE
Oxybutynin: Tx overactive bladder
Dicyclomine: used for IBS
Glycopyrolate: used for sialorhea, surgical HR control
Ipratropium: Used for COPD, Asthma (bronchodilation)

63
Q

Parasympathetics ( Cholenergics )
Direct Agonists

A

Bethancol: Used for urinary retention.
Carbachol: decr IOP in galucoma.
Methacholine: used to induce bronchoconstriction to test for asthma.
Pilocarpine: Sjorgen Syndrome (salivation), Dry eyes (lacrimation), sweat (Dx of cystic fibrosis)

64
Q

Parasympthetics (Cholenergics)
Indirect Agonist

A

Increase Ach, Inhibits Ach Esterase that normally breaks down Ach thereby increasing Ach levels.
Physostigmine: used in Atropine OD, Belladona alkaloid poisoning (deadly night shade)
Pyridostigmine: Tx Mysthenia gravis
Edriphonium: used in Dx of Mysthenia gravis
Donepezil: Tx Alzhimers.

65
Q

Entacapone

A

COMT inhibitor
Prevent Dopamine breakdown to 3MT
Used for parkinsons disease
Usually added to therapy after levodopa and carbidopa combo when symptoms still presist

66
Q

Selegiline, Resegiline

A

MAO-B inhibitors
Prevent dopamine breakdown to DOPAC
Used in parkinsons disease

67
Q

Amantadine

A

Inhibits dopamine reuptake
Used for parkinsons disease

68
Q

Bromocriptine, Pramipaxole, Ropinirole

A

Dopamine agonist
Increase level of dopamine in the synaptic cleft, binds to and stimulates post synaptic dopamine receptors.
Used for parkinsons disease

69
Q

Carbidopa

A

Blocks peripheral Dopa decarboxylase to increase dopamine levels in brain.
Used for parkinsons disease.
S/E: Nausea, Vomitting.

70
Q

Levodopa

A

CNS agent, converts to dopamine in brain
Carbidopa is given with levodopa that prevents its peripheral conversion to dopamine allowing it to go into the brain.
Used for parkinsons disease.

71
Q

Lithium

A

Modulation of phospho inostol pathway
Mood stablizer, used in bipolar disorder
S/E:
Nephrogenic DI (V2 aquaporin damage)
Hyper/Hypo thyroidism
Causes Ebstien anomaly in unborn child of mother taking lithium
CKD (increase Cr)

72
Q

Valproic Acid

A

Increase Na+ channel inactivation
Increase GABA conc
Used in bipolar disorder
S/E:
Thrombocytopenia
LFT elevation
Neural tube defects
Pancreatitis

73
Q

Lamotrigine

A

Glutamate inhibition, Voltage gated Na+ channel inhibition
Used for depression in bipolars, Siezures
S/E:
Steven-Jhonson syndrome
Malignant appearing rash

74
Q

Carbamazipine

A

Blocks Na+ channels (increases refractory period)
Used for Mania in bipolars, Trigeminal neuralgia
S/E:
Agranulocytosis ( decrse WBC, Neutropenia)
SIADH
Potent P450 inducer

75
Q

Ethosuximide

A

Decrease T-type Ca+2 channel
Used for absence siezures
S/E: steven johnson syndrome

76
Q

Phenytoin

A

Decrease voltage gated Na+ channels
S/E:
Zero order kinetics (eliminated at const rate)
P450 inducer
Gingival hyperplasia
Fetal hydantoin syndrome

77
Q

Valporate

A

Decrease voltage gated Na+ channel + Increase GABA
1st line for general or partial tonic clonic siezures
S/E:
Anemia
Hepatotoxicity
Pancreatitis
Spinabifida

78
Q

Benzos & Barbiturates

A

Increase GABAa
Benzos: Increase frequency of Cl- channels
BB; Increase duration of Cl- channels
Indication Siezures (abortive)

Barbiturates are CNS depressants > Respiratory depression > inc CO2 , decr O2,
A-a gradient is Normal.

79
Q

Tigabine & Vigabatrin

A

Increase GABA activity

80
Q

Topiramate

A

Decrease voltage gated Na+ channel
Prevents siezures

81
Q

Oseltamivir, Zanamivir

A

Neuraminudase inhibitor
Only effective within 48hrs of symptom onset
Used for treatment of Influenza.

82
Q

Acyclovir, Valcyclovir, Famicyclovir

A

Guanine analogs that phosphorylates acyclovir to terminate the growing chain by inhibiting viral DNA polymerase
Resistance via mutated Thymidine Kinase.
Acyclovir is used for treatment of Herpes.

S/E: obstructive crystalline nephropathy if adequate hydration is not provided.

83
Q

Foscarnet, Cidofavir

A

Inhibits viral DNA polymerase
S/E: Nephrotoxicity
Foscarnet is pyrophosphate analog

84
Q

Foscarnet, Cidofavir

A

Inhibits viral DNA polymerase
S/E: Nephrotoxicity
Foscarnet is pyrophosphate analog and does not require activation by body emzymes.

85
Q

Interferon alpha

A

Has antiviral properties internally produced by body

inhibition of protein synthesis, inactivation of viral RNA, and enhancement of phagocytic and cytotoxic mechanisms

86
Q

Hepatitis-C Drugs

A

Simepravin: NS3A/4B protease inhibitor
Ledipasvir: NS5A inhibitor
Both prevent fusion and uncoating

Sofobosvir: NS5B inhibitor
Inhibit RNA dependant DNA polymerase
Inhibit transcription and replication

87
Q

NRTIs
HIV antivirals

A

Abacavir, Didanosine (pancreatitis), Ziduvidine (anemia), Lamivudine, Tenofivir, Stavudine, Emtricitabine

Blocks reverse transcriptase prevent replication by preventing 3’ to 5’ phosphodiestrase bonds in growing DNA chain
S/E:
Peripheral neuropathy
Bone marrow suppression
Lactic acidosis
Pancreatitis (Didanosine specific)
Anemia (Ziduvidine specific)

88
Q

NNRTIs
HIV antivirals

A

“DEN”
Delaviridine, Efavirnez, Nevirapine
Binds to different site of reverse transcriptase and creates hydrophobic pocket which slows DNA synthesis
Doesnot require phosphorylation
Not effective against HIV-2 reverse transcriptase
S/E:
Hepatoxicity
Vivid dreams (specific to Efavirenz)
Efavirenz + Delaviridine C/I in pregnancy

89
Q

Protease inhibitors
HIV antivirals

A

“ A I R “
Atazanvir , Indanavir , Ritonavir
Blocks HIV proteases ability to cleave precursors effectively blocking viral maturation
S/E:
Hyperglycemia , GI side effects
Lipodystrophy
Nephropathy (specific to Indanavir)
P 450 inhibition (specific to Ritonavir)

90
Q

Integrase inhibitor
HIV antivirals

A

“ R E D “
Raltegravir , Elvitegravir , Dolutegravir
Blocks integrase ability to incorporate viral DNA into host genome.
S/E:
Increase Creatine Kinase (CK)

91
Q

Fusion inhibitors
HIV antivirals

A

Enfuviritide:
Binds GP41 , prevents penetration , GP41 on envelope

Maraviroc:
Binds CCR5 , prevents attachment , CCR5 on macrophages

92
Q

AZOLES
Clotrimazole, Fluconazole, Itraconazole, Ketoconazole

A

Inhibits 14 alpha demethylase
Prevents ergosterol synthesis

93
Q

Terbinafine

A

Inhibits squalene Epoxidase
Inhibits squalene conversion to squalene epoxide in fungus

94
Q

Amphotericin-B

A

Creates holes in ergosterol & destroying fungal cell membrane
S/E:
Phlebitis
Fever, Chills, Fatigue
Nephrotoxicity (alters permiability & flow in nephron) ( alteration of electrolytes e.g Mg+2 , K+ )

95
Q

Nystatin

A

Used in oral thrush
Tears holes in ergosterol destroying fungal cell membrane

96
Q

Echinocandins
( Capsofungin )

A

Inhibits Betaglucans synthase
Inhibits cell wall synthesis

97
Q

Flucytosiene

A

Inhibits DNA of fungal cells
Wedges itself in the DNA and converted into 5-FU by cytosiene deaminase

98
Q

Gresiofluvin

A

Microtubule inhibitors
Antifungal

99
Q

Metronidazole

A

diffuses into the organism, inhibits protein synthesis by interacting with DNA, and causes a loss of helical DNA structure and strand breakage

100
Q

Albendazole

A

Broad spectrum antihelmenthic

inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules

101
Q

Mebendazole

A

inhibiting the production of microtubules via binding to colchicine binding-site of β-tubulin and thereby blocking polymerization of tubulin dimers in the intestinal cells of parasites

102
Q

Penicillins

A

inhibits cell wall synthesis by inhibiting peptidoglycan synthesis, particularly the transpeptidation reaction.

3 mechanism for resistance:
(1) enzymatic degradation of antibacterial drugs, (2) alteration of bacterial proteins that are antimicrobial targets
(3) changes in membrane permeability to antibiotics.

S/E: Hives , Rash , Itching , Anaphylaxis.

103
Q

Cephalosporins

A

Closely related to penicillins
Bacteriocidal , Inhibits cell wall synthesis

1st Gen: Az Ale ( cefAZolin , cefALExin)
3rd Gen: 3 Tri , Tax , Taz
( cefTRIaxone , cefTAXime , cefTAZidime )
4th Gen: Cefepime ( covers pseudomonas )
5th Gen: Ceftaroline

S/E:
Hypersenstivity reaction
Autoimmune hemolytic anemia
Disulfram like reaction
Vit-K deficiency
Nephrotoxic synergy with aminoglycosides

104
Q

Aminoglycosides

gentamicin, tobramycin, streptomycin, neomycin, and paromomycin

A

Prevent protien translation

act by binding to the aminoacyl site of 16S ribosomal RNA within the 30S ribosomal subunit

S/E: Nephrotoxicity & Otoxicity

105
Q

Macrolides

erythromycin, clarithromycin, azithromycin, fidaxomicin and telithromycin

A

Macrolies inhibit bacterial protein synthesis

bind the bacterial 50S ribosomal subunit causing the cessation of bacterial protein synthesis.

S/E: nausea, vomiting, abdominal pain, and diarrhea
Rare S/E: Hepatoxicity, angioedema, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

106
Q

Fomepizole

A

Inhibits alcohol dehydrogenase
Used to treat methanol and ethylene glycol intoxication.

107
Q

Steady State of Drugs

A

A state in which rate of elimination of drug is equal to rate of administration.
Rate of elimination is quantified by half life
In general it takes 5 half lifes to get to steady state conc and about slightly more than 3 halflifes to get to 90% steady state level.

108
Q

Acetazolamide

A

Works on PCT
Carbonic Anhydrase inhibitor, prevents Bicarbonate reabsorption.
Used for Galucoma, Metabolic Alkalosis, Altitude Sickness

S/E:
Hyperchloremic metabolic acidosis, ammonium toxicity, sulfa drug allergy

109
Q

Mannitol

A

Works on PCT
Osmotic diuretic, Increases tubular fluid osmolarity
Used for Shock, drug overdose, to decrease intracranial/intraocular pressure

S/E: Pulmonary Edema, Dehydration (contraindicated in CHF)

110
Q

Furosemide

A

Loop Diuretic works on Loop of Henle

Prevents cotransport of Na+, K+, and Cl- in thick ASCENDING loop, Increase Ca2+ excretion, stimulates PGE release (vasodilator effect on the afferent arteriole); inhibited by NSAIDS.

Used for CHF, Cirrhosis, Nephrotic syndrome, Pulmonary Edema, Hypertension, Hypercalcemia
S/E:
Ototoxicity, Hypokalemia, Metabolic Alkalosis, Dehydration, Sulfa drug allergy, Hyperuricemia (increase urate reabsorption)

111
Q

Ethacrynic Acid

A

Phenoxyacetic acid derivative (not a sulfonamide), prevents cotransport of Na+, K+ and 2 Cl- in thick ascending loop.

S/E:
Ototoxicity (reversible), Hypokalemia, Metabolic Alkalosis, Hypomagnesemia

112
Q

Hydrochlorothiazide (HCTZ)

A

Works on DCT
­Incr Ca+2, Incr HCO3-, Incr PH,
decr K+, decr Urinary Ca+2

Inhibit transport of Na+ and Cl- into cells of the DCT, enhances Ca2+ reabsorption
(Ca2+ and Na+ compete for ATP dependent reabsorption in the DCT)
Used for Hypertension, CHF, Idiopathic Hypercalciuria, Nephrogenic Diabetes Insipidus

S/E: Hypokalemic Metabolic Alkalosis, Hyponatremia, Hyperglycemia, Hyperlipidemia, Hyperuricemia, Hypercalcemia, Sulfa drug allergy

113
Q

Spironolactone & Epirelinone

A

K+ sparing diuretics
Competitive Aldosterone receptor antagonist in the cortical collecting tubule.
Used for Hyperaldosteronism, K+ depletion, CHF.

S/E:
Hyperkalemia (can lead to Arrhythmias), Gynecomastia, Antiandrogen effects (Eplerenone less likely to cause Gynecomastia)

114
Q

Amiloride & Traimterene

A

K+ sparing diuretics
Work on Cortical Collecting Tubule

Block Na+ channels in the cortical collecting tubule; Amilioride causes increased Ca2+ reabsorption to treat Ca2+ based Nephrolithiasis
Used for Hyperaldosteronism, K+ depletion, CHF

S/E : Hyperkalemia (can lead to Arrhythmias)

115
Q

ACE Inhibitors
Captopril, Lisinopril, Enalapril, Ramipril

A

All have “PRIL” in their name
Inhibit Angiotensin-converting enzyme (ACE), and preventing inactivation of Bradykinin

Used for Hypertension, CHF, Diabetic Renal disease. Prevent unfavorable heart remodeling as a result of chronic hypertension.

S/E :
“CAPTOPRIL”
Cough
Angioedema
Proteinuria
Taste changes
hypOtension
Pregnancy problems (fetal renal damage)
Rash
Increased Renin
Low Angiotensinogen II (AT II) causing Hyperkalemia.

116
Q

Emicizumab

A

Biospecfic monoclonal antibody
Mimics the activity of factor VIII, binds factor IXa & factor X and brings them close to activate factor X (Xa).
Used for bleeding in Hemophilia A (factor VIII def)

117
Q

Dantrolene

A

Used to treat Malignant Hyperthermia
It directly inhibits intracellular calcium release from abnormal Ryanodine receptors (RYR1)

118
Q

Rasburicase

A

Recombinant version of Urate oxidase
Converts Uric acid to Allantoin, which is more soluble and far less likely to precipitate in kidney than uric acid.
Used along with chemotherapy for Tumor Lysis Syndrome for Hyperuricemia caused by incr cell turnover rate.

119
Q

Azathioprine

A

Anti-cancer drug
S-phase inhibitor
↓ de novo purine synthesis
Activated by HGPRT
Converted to 6-Merceptopurine
Metabolized by Xanthine Oxidase

C/I with Xanthine Oxidase inhibitors
(Allopurinol/ Febuxostat)

120
Q

6-Merceptopurine

A

Anti cancer drug
S-phase inhibitor
↓ de novo purine synthesis
Activated by HGPRT
Metabolized by Xanthine Oxidase.

C/I with Xanthine Oxidase inhibitors
(Allopurinol/ Febuxostat)

121
Q

Anti cancer drugs
M-phase Inhibitors

A

Microtubule inhibitors

– Vincristine/ Vinblastine (binds to beta tubulin prevents polymerization).
S/E: Neurotoxicity.

– Paclitaxel (hyperstablizes M-phase).
S/E: Neuropathy.

– Eribulin (binds hi affinity ends of microtubules)
S/E: Arthralgias.

122
Q

Anti Cancer Drugs
G-1 Phase Inhibitors

A

Mechanism: Inhibits DNA cross linking.

– Cisplatin : S/E- Ototoxicity, Nephrotoxicity.
Rx : Amphostine , Saline.

– Busulfan : S/E- Pulmonary Fibrosis

– Cyclophosphamide: Guanine liver bioactivation
S/E: Hemorhagic Cystitis , SIADH
Rx: Mesna

– Carmustine : Crosses BBB, Brain bioactivation
S/E : CNS toxicity

123
Q

Anti Cancer Drugs
S-Phase Inhibitors

A

S-phase synthesises DNA

– Cladrabine: Purine analog,
S/E; Neuro/Nephro toxicity.

– Cytarabine: Pyramidine analog
S/E: Pancytopenia.

– 5-FU : Pyramidine analog
Inhibits Thymidyl Synthase
S/E: Hand foot syndrome

– Methotrexate : Inhibits dihydrofolate reductase
S/E: Myelosupression
Rx : Leucovorin

Other s-phase inhibitors like azathioprine, 6-merceptopurine & hydroxyurea have their own cards.

124
Q

Anti Cancer Drugs
G-2 Phase Inhibitors

A

Teniposide & Etoposide :
Inhibits Topoisomerase 2.

Topotecan & Irinotecan :
Inhibits Topoisomerase 1.

125
Q

Anti Tumor Antibiotics

A

Doxorubicin & Danorubicin :
Intercalates DNA
S/E: Dilated Cardiomyopathy.
Rx: Dexarazone

Bleomycin : Generates Free radicals
S/E: Pulmonary Fibrosis

126
Q

OCP Note

A

OCP are contraindicated in women over 35yrs old who are smokers because of increase risk of thromoboembolitic event (i.e pulmonary embolisim)

127
Q

Hep-C therapy?

A

Ribavirin: Nucleotide synthesis inhibitor.

Sofosbuvir: RNA-Dependent RNA-polymerase inhibitor.

Simeprevir: Protease Inhibitor.

Ledipasvir: NS5A Inhibitor.

128
Q

Linezolid

A

Linezolid blocks bacterial protein synthesis by binding 50S ribosomal subunit. It has activity against gram-(positive) bacteria.

129
Q

Penicillin

A

Penicillin inhibits bacterial cell wall synthesis by binding transpeptidase enzyme. This primarily prevents (peptidoglycan crosslinking).

130
Q

Vancomycin

A

Vancomycin inhibits cell wall synthesis by binding D-alanine-D-alanine residues. This primarily prevents (incorporation of new cell wall subunits) (acts at an earlier stage of cell wall formation than penicillin).

131
Q

Azithromycin, clarithromycin, erythromycin are examples of what class of antibiotics?

A
  • Macrolides
  • They inhibit bacterial protein synthesis by binding the 50S ribosomal
    subunit.
132
Q

Ciprofloxacin, levofloxacin, and moxifloxacin are examples of what class of antibiotics?

A

Fluoroquinolones

They block bacterial synthesis of DNA by inhibiting (DNA gyrase [topoisomerase II]) and (topoisomerase IV).

133
Q

Vancomycin is used for which organism and what is the mechanism for its resistance?

A

Vancomycin is active against gram-(positive) bacteria

Primary mechanism of resistance to vancomycin: Substitution of the terminal D-alanine with D-lactate (prevents vancomycin binding).

Vancomycin is often used in the treatment of methicillin-resistant staphylococci.

134
Q

Sevelamer

A

Sevelamer (a phosphate binder) is used to manage hyperphosphatemia in chronic kidney disease.

135
Q

Which class of antidiabetic drugs decreases insulin resistance by activating peroxisome proliferator–activated receptor gamma?

A

Thiazolidinediones (eg, pioglitazone).

136
Q

Acarbose

A

Inhibits (alpha-glucosidase) located in the intestinal brush border. This leads to decreased postprandial absorption of glucose.

137
Q

What is the hematologic adverse effect associated with thionamides (eg, methimazole, propylthiouracil)?

A

Drug-induced neutropenia/agranulocytosis.

Thionamides are used in the treatment of hyperthyroidism.

Methimazole and propylthiouracil are indicated for the treatment of hyperthyroidism. They inhibit (thyroid peroxidase).

138
Q

Name 2 classes of antidiabetic drugs that inhibit the potassium channel on the pancreatic beta cell membrane:

A
  1. Sulfonylureas (eg, glyburide, glipizide)
  2. Meglitinides (eg, repaglinide)

They induce insulin release independent of blood glucose concentrations, which increases the risk of (hypoglycemia).

139
Q

Antidiabetic drug that decreases hepatic gluconeogenesis by inhibiting mitochondrial glycerophosphate dehydrogenase?

A

Metformin (reduces the availability of substrates for gluconeogenesis)

This drug has a (low) risk of hypoglycemia (because it does not increase endogenous insulin secretion).

140
Q

What is the mechanism of action of the following anesthetics?

A
  1. Lidocaine: Blocks voltage gated Na channels
  2. Propofol: Potentiates GABA A receptor
  3. Ketamine: Inhibits NMDA receptors
141
Q

Denosumab

A

In the treatment of osteoporosis, denosumab binds RANK-L and prevents its interaction with the RANK receptor, resulting in decreased osteoclast differentiation/activity and decreased bone resorption.

Rapid Review Step 1 (24 decks)

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