Pharma Flashcards
QT Prolongating Drugs
- 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)
Sulfonylureas
Meglitinides
- 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
Biguanides
Metformin
- Stimulate AMPK & inhibit mitochondrial gluconeogenesis, ↓ hepatic glucose production & ↑ peripheral glucose uptake, Increases insulin senstivity.
S/E:
- Diarrhea
- Lactic acidosis
Thiazolidinediones
Pioglitazone
- Activate transcription regulator PPAR-γ, ↓ insulin resistance
S/E:
- Fluid retention/heart failure
- Weight gain
GLP-1 agonists
Exenatide
Liraglutide
- ↑ Glucose-dependent insulin secretion, ↓ glucagon secretion, delayed gastric emptying
S/E:
- Pancreatitis
- Weight loss
DPP4 inhibitors
Sitagliptin
Saxagliptin
- ↑ Endogenous GLP-1 & GIP levels
- S/E: Nasopharyngitis
SGLT-2 inhibitors
Canagliflozin
Dapagliflozin
- ↑ Renal glucose excretion
S/E:
- Urinary tract infections
- Hypotension
Selective estrogen receptor modulators (SERMs)
- 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)
Bisphosphonates
- Alendronate, Risedronate
- Are used to treat osteoporosis and act by inhibiting osteoclast-mediated bone resorption.
Denosumab
- Binds RANKL & inhibits binding to RANK
- Reduces differentiation & survival of osteoclasts
- Used in Osteoporosis
Recombinant PTH analog (Teriparatide)
- (Teriparatide)
- Stimulates maturation of pre-osteoblasts into bone-forming osteoblasts
- Increases gastrointestinal calcium absorption & renal tubular calcium reabsorption
Statins
- HMG Co A Reductase Inhibitor , LDL receptor upregulation
- Atorvastatin, Rosuvastatin, Simvastatin
- Decrease LDL
- Increase HDL
- Decrease Serum Triglycerides
- Pravastatin is only statin that undergoes renal excretion
B-Blockers Overdose
- 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.
Bupropion
- Inhibit reuptake of NE and dopamine.
- Used to treat MDD (1st line)
- No sexual side effects
- Increase dosage have high risk for seizure
- C/I in seizure disorder, bulimics and anorexia
Ramelteon
- Melatonin agonist
- Used for insomnia in elderly, it has lowest side effects among all the sedatives.
Ipratropium
- Muscarinic Antagonist
- Competitively block muscarinic receptor to prevent
- Bronchoconstriction
- Used in Asthma
Beclomethasone, Prednisone
- Corticosteroids
- Inhibit Leukotriene Synthesis
- Reduce inflammation leads to bronchodilation
- Used in COPD & Asthma
S/E:
- Osteoporosis,
- Cushingoid reaction,
- Glucose intolerance,
- Infection ,
- HTN,
- Cataracts
Methylxanthines
- Theophylline
- Inhibits PDE > dec cAMP Hydrolysis (inc cAMP) promoting bronchodilation
- Used for Asthma
- S/E: Cardiotoxicity, Neurotoxicity
Cromolyn
- Prevent release of mediators from mast cells
- Used in asthma prophylaxis
Zileuton , Zafrilukast, Montelukast
- Anti-leukotrienes
- 5-lipoxygenase inhibitor → inhibit conversion of arachidonic acid to leukotrienes → prevents bronchoconstriction & inflammatory cell infiltrate
- Used for aspirin induced asthma
Diphenhydramine, Chlorpheniramine
- 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)
Guaifenesin
- Expectorant
- Removes excess sputum but does not suppress cough reflex
- Used for minor URI, Common cold w/cough
N-acetyl cysteine
- Expectorant
- Loosens mucus plugs by breaking di sulfide bonds
- Used for Cystic fibrosis, antitode for Acetaminophen OD
Loratadine, Fexofenadine, Desloratadine, Cetirizine
- 2nd Gen H-1 blockers
- Less sedating than 1st gen because of decreased entry into CNS
- Used for Allergy
Bosentan
- Competitively antagonizes endothelium-1 receptors decreasing pulmonary vascular resistance
- Used for Pulmonary HTN
Pseudoephedrine, Phenylephrine
- 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
Salmeterol
- B-2 agonist : relaxes bronchial smooth muscles
- Long Acting (LABA) used for prophylaxis of Asthma/COPD
- S/E: Tremor & Arrhythmia
Albuterol
- B-2 agonist : relaxes bronchial smooth muscles
- Used for Acute exacerbation of Asthma
Isoproterenol
- Non-specific Beta agonists, relaxes bronchial smooth muscles (B2)
- Used for Bronchoconstriction due to sympathetic tone
- S/E: Tachycardia
Methacholine
- Muscarinic receptor Agonist
- Used in asthma challenge test
Dextromethorphan
- Anti tussive, Antagonizes NDMA & Glutamate Receptors
- S/E: Mild Opioid effect so mild abuse potential
Desmopressin DDAVP
- 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
Fibrates
- (Fenofibrate, Gemfibrozil)
- Upregulates Lipoprotein Lipase
- Results in increase oxidation of FA
- Inhibit cholesterol 7 alpha- hydroxylase
- Increase risk of cholesterol gallstones
Ursodiol
- Decrease cholesterol secretion into bile thereby preventing the cholesterol gallstones formation
- 2nd line for cholelithiasis after cholecystectomy (1st line)
Heparin
- Unfractioned Heparin, LMWH
- Prevent Factor X → Xa
- Antitode Protamine Sulphate
- Can cause Heparin induces Thrombocytopenia
Warfarin
- 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.
Factor Xa inhibitors
- Inhibits factor X → Xa
- Direct: Rivaroxaban, Apixaban
- Indirect: parinaux
Agatroban, Bivalirudin
- Direct thrombin Inhibitors
- Inhibit prothrombin to thrombin conversion
- Factor - II → IIa inhibition
Clopidogrel
- 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
HydroxyUrea
- Inhibit Ribonucleotide Reductase
- Decrease DNA synthesis
- Used in Sickell cell anemia & CML
- Increase HbF
- S/E: long use causes Myelosuppression
Ruburicase/ Pioglitacase
- 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
Fludocortisone
- Steroid acts as Aldosterone
- Used in 21-hydroxylase deficiency and in patients with low aldosterone
Sevelamer
- Non absorbable phospate binder that prevents phosphate absorbtion from GI tract
Methimazole
- 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
PTU (Propiothiyouracil)
- 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
Liothyroinine/ Levothyroxine
- Liothyronine: T3
- Levothyroxine: T4
Patiromer
- Chelator in GI tract
- S/E: Diarrhea, GI disturbance, Hypokalemia
Acarbose/ Miglitol
- Antidiabetic
- Inhibits intestinal brush border A-glucosidase
- S/E: Diarrhea, Malabsorbtion (Blunting of GI brush borders)
Cinacalcet
- Used for hypocalcemia due to CKD or PTH
- Increases Ca+2 receptor senstivity, when it senses calcium provides feedback inhibtion to PTH.
Tolvaptan
- ADH receptor antagonist (reversible)
- Used to treat SIADH
Demclocycline
- Tetracycline
- Damages ADH receptor (irreversible)
Rifampin
- Inhibits DNA dependent 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
INH (Isoniazid)
- 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
Pyrazinamide
- Accumulation of pyrazonic acid, decrease proton motive force, decrease EN2F (X)
- Used in TB (negotiable med)
S/E:
- Hepatotoxic
- Hyperuricemia
- C/I in pregnancy
Ethambutol
- Inhibits arabinosyl transferase (decrease cell wall production)
- Used in TB (negotiable med)
S/E:
- Optic neuritis
- C/I in SLE
Mofetil, Mycophenolate
- Affects purine pathway, IMP-dehydrogenase
S/E:
- GI problems
- Pancytopenia
Eculizumab
Monoclonal antibody affecting complement especially C-5
Omalizumab
- Monoclonal antibody
- Prevents IgE binding to mast cells by blocking the receptor, prevents degranulation
- Used in people with allergy
Sucralfate
- Attaches on top of ulcer provides physical protection and allows HCO3– to re-establish the PH gradient and allows healing.
- S/E: Diarrhea
Sulfasalazine
- Combo of Antibacterial + Anti inflammatory
- Sulphapyridine + 5-aminosalicyclic acid (aspirin)
- Requires activation by colonic bacteria
S/E:
- Diarrhea → Malabsorption
- Reversible Oligospermia
Metoclopramide
- 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, Akathisia, Parkinsonian symptoms)
Anti-parasympatheitics
→ Anti-Cholinergic , Anti-muscarinic
- Atropine: Rx cholinergic poisoning, unstable bradycardia
- Scopolamine: Tx Motion Sickness
- Benztropine: Tx Extrapyramidal SE
- Trihexyphenidyl: Tx Extrapyramidal SE
- Oxybutynin: Tx overactive bladder
- Dicyclomine: used for IBS
- Glycopyrrolate: used for sialorrhea, surgical HR control
- Ipratropium: Used for COPD, Asthma (bronchodilation)
Parasympathetics ( Cholinergic )
Direct Agonists
- Bethanechol: Used for urinary retention.
- Carbachol: decrease IOP in glaucoma.
- Methacholine: used to induce bronchoconstriction to test for asthma.
- Pilocarpine: Sjogren Syndrome (salivation), Dry eyes (lacrimation), sweat (Dx of cystic fibrosis)
Parasympathetics (Cholinergic)
Indirect Agonist
- Increase Ach, Inhibits Ach Esterase that normally breaks down Ach thereby increasing Ach levels.
- Physostigmine: used in Atropine OD, Belladonna alkaloid poisoning (deadly night shade)
- Pyridostigmine: Tx Myasthenia gravis
- Edrophonium: used in Dx of Myasthenia gravis
- Donepezil: Tx Alzheimer’s.
Entacapone
- COMT inhibitor
- Prevent Dopamine breakdown to 3MT
- Used for parkinsons disease
- Usually added to therapy after levodopa and carbidopa combo when symptoms still presist
Selegiline, Resegiline
- MAO-B inhibitors
- Prevent dopamine breakdown to DOPAC
- Used in Parkinson’s disease
Amantadine
- Inhibits dopamine reuptake
- Used for Parkinson’s disease
Bromocriptine, Pramipaxole, Ropinirole
- Dopamine agonist
- Increase level of dopamine in the synaptic cleft, binds to and stimulates post synaptic dopamine receptors.
- Used for Parkinson’s disease
Carbidopa
- Blocks peripheral Dopa decarboxylase to increase dopamine levels in brain.
- Used for Parkinson’s disease.
- S/E: Nausea, Vomiting.
Levodopa
- 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 Parkinson’s disease.
Lithium
- Modulation of phospho inositol pathway
- Mood stabilizer, used in bipolar disorder
S/E:
- Nephrogenic DI (V2 aquaporin damage)
- Hyper/Hypothyroidism
- Causes Epstein anomaly in unborn child of mother taking lithium
CKD (increase Cr)
Valproic Acid
- Increase Na+ channel inactivation
- Increase GABA conc
- Used in bipolar disorder
S/E:
- Thrombocytopenia
- LFT elevation
- Neural tube defects
- Pancreatitis
Lamotrigine
- Glutamate inhibition, Voltage gated Na+ channel inhibition
- Used for depression in bipolars, Seizures
S/E:
- Steven-Johnson syndrome
- Malignant appearing rash
Carbamazipine
- Blocks Na+ channels (increases refractory period)
- Used for Mania in bipolars, Trigeminal neuralgia
S/E:
- Agranulocytosis ( decrease WBC, Neutropenia)
- SIADH
- Potent P450 inducer
Ethosuximide
- Decrease T-type Ca+2 channel
- Used for absence seizures
- S/E: steven Johnson syndrome
Phenytoin
- Decrease voltage gated Na+ channels
S/E:
- Zero order kinetics (eliminated at const rate)
- P450 inducer
- Gingival hyperplasia
- Fetal hydantoin syndrome
Valporate
- Decrease voltage gated Na+ channel + Increase GABA
- 1st line for general or partial tonic-clonic seizures
S/E:
- Anemia
- Hepatotoxicity
- Pancreatitis
- Spina bifida
Benzos & Barbiturates
- Increase GABAa
- Benzos: Increase frequency of Cl- channels
- BB; Increase duration of Cl- channels
- Indication Siezures (abortive)
- Barbiturates are CNS depressants → Respiratory depression → increase CO2 , decrease O2,
- A-a gradient is Normal.
Tigabine & Vigabatrin
Increase GABA activity
Topiramate
- Decrease voltage gated Na+ channel
- Prevents siezures
Oseltamivir, Zanamivir
- Neuraminidase inhibitor
- Only effective within 48-hrs of symptom onset
- Used for treatment of Influenza.
Acyclovir, Valcyclovir, Famicyclovir
- 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.
Foscarnet, Cidofavir
- Inhibits viral DNA polymerase
- S/E: Nephrotoxicity
- Foscarnet is pyrophosphate analog
Foscarnet, Cidofavir
- Inhibits viral DNA polymerase
- S/E: Nephrotoxicity
- Foscarnet is pyrophosphate analog and does not require activation by body emzymes.
Interferon alpha
- Has antiviral properties internally produced by body
- Inhibition of protein synthesis, inactivation of viral RNA, and enhancement of phagocytic and cytotoxic mechanisms
Hepatitis-C Drugs
- Simepravin: NS3A/4B protease inhibitor
- Ledipasvir: NS5A inhibitor
- Both prevent fusion and uncoating
- Sofosbuvir: NS5B inhibitor
- Inhibit RNA dependent DNA polymerase
- Inhibit transcription and replication
NRTIs
HIV antivirals
- Abacavir, Didanosine (pancreatitis), Zidovudine (anemia), Lamivudine, Tenofovir, Stavudine, Emtricitabine
- Blocks reverse transcriptase prevent replication by preventing 3’ to 5’ phosphodiesterase bonds in growing DNA chain
S/E:
- Peripheral neuropathy
- Bone marrow suppression
- Lactic acidosis
- Pancreatitis (Didanosine specific)
- Anemia (Zidovudine specific)
NNRTIs
HIV antivirals
→ “DEN”
- Delavirdine, Efavirenz, Nevirapine
- Binds to different site of reverse transcriptase and creates hydrophobic pocket which slows DNA synthesis
- Doesn’t require phosphorylation
- Not effective against HIV-2 reverse transcriptase
S/E:
- Hepatoxicity
- Vivid dreams (specific to Efavirenz)
- Efavirenz + Delavirdine C/I in pregnancy
Protease inhibitors
HIV antivirals
→ “ A I R “
- Atazanavir , Indinavir , Ritonavir
- Blocks HIV proteases ability to cleave precursors effectively blocking viral maturation
S/E:
- Hyperglycemia , GI side effects
- Lipodystrophy
- Nephropathy (specific to Indinavir)
- P 450 inhibition (specific to Ritonavir)
Integrase inhibitor
HIV antivirals
→ “ R E D “
- Raltegravir , Elvitegravir , Dolutegravir
- Blocks integrase ability to incorporate viral DNA into host genome.
- S/E : Increase Creatine Kinase (CK)
Fusion inhibitors
HIV antivirals
- Enfuvirtide:
Binds GP41 , prevents penetration , GP41 on envelope - Maraviroc:
Binds CCR5 , prevents attachment , CCR5 on macrophages
AZOLES
Clotrimazole, Fluconazole, Itraconazole, Ketoconazole
- Inhibits 14 alpha demethylase
- Prevents ergosterol synthesis
Terbinafine
- Inhibits squalene Epoxidase
- Inhibits squalene conversion to squalene epoxide in fungus
Amphotericin-B
- Creates holes in ergosterol & destroying fungal cell membrane
S/E:
- Phlebitis
- Fever, Chills, Fatigue
- Nephrotoxicity (alters permeability & flow in nephron) ( alteration of electrolytes e.g. Mg+2 , K+ )
Nystatin
- Used in oral thrush
- Tears holes in ergosterol destroying fungal cell membrane
Echinocandins
( Capsofungin )
- Inhibits Beta glucans synthase
- Inhibits cell wall synthesis
Flucytosiene
- Inhibits DNA of fungal cells
- Wedges itself in the DNA and converted into 5-FU by cytosine deaminase
Gresiofluvin
- Microtubule inhibitors: Antifungal
Metronidazole
Diffuses into the organism, inhibits protein synthesis by interacting with DNA, and causes a loss of helical DNA structure and strand breakage
Albendazole
- Broad spectrum anthelminthic
- Inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules
Mebendazole
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
Penicillins
- 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.
Cephalosporins
- Closely related to penicillin’s
- Bactericidal , 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:
- Hypersensitivity reaction
- Autoimmune hemolytic anemia
- Disulfiram like reaction
- Vit-K deficiency
- Nephrotoxic synergy with aminoglycosides
Aminoglycosides
gentamicin, tobramycin, streptomycin, neomycin, and paromomycin
- Prevent protein translation
- Act by binding to the aminoacyl site of 16S ribosomal RNA within the 30S ribosomal subunit
- S/E: Nephrotoxicity & Ototoxicity
Macrolides
erythromycin, clarithromycin, azithromycin, fidaxomicin and telithromycin
- Macrolides 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.
Fomepizole
- Inhibits alcohol dehydrogenase
- Used to treat methanol and ethylene glycol intoxication.
Steady State of Drugs
- 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.
Acetazolamide
- Works on PCT
- Carbonic Anhydrase inhibitor, prevents Bicarbonate reabsorption.
- Used for Glaucoma, Metabolic Alkalosis, Altitude Sickness
- S/E: Hyperchloremic metabolic acidosis, ammonium toxicity, sulfa drug allergy
Mannitol
- 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)
Furosemide
- 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)
Ethacrynic Acid
- 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
Hydrochlorothiazide (HCTZ)
- Works on DCT
- Increase Ca+2, Increase HCO3-, Increase PH,
decrease K+, decrease 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
Spironolactone & Epirelinone
- 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)
Amiloride & Traimterene
- 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)
ACE Inhibitors
Captopril, Lisinopril, Enalapril, Ramipril
- 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.
Emicizumab
- Bio-specific monoclonal antibody
- Mimics the activity of factor VIII, binds factor IX a & factor X and brings them close to activate factor X (X a).
- Used for bleeding in Hemophilia A (factor VIII def)
Dantrolene
- Used to treat Malignant Hyperthermia
- It directly inhibits intracellular calcium release from abnormal Ryanodine receptors (RYR1)
Rasburicase
- 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 increase cell turnover rate.
Azathioprine
- 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)
6-Merceptopurine
- 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)
Anti cancer drugs
M-phase Inhibitors
- Microtubule inhibitors
- Vincristine/ Vinblastine (binds to beta tubulin prevents polymerization).
S/E: Neurotoxicity. - Paclitaxel (hyper stabilizes M-phase).
S/E: Neuropathy. - Eribulin (binds hi affinity ends of microtubules)
S/E: Arthralgias.
Anti Cancer Drugs
G-1 Phase Inhibitors
- Mechanism: Inhibits DNA cross linking.
- Cisplatin : S/E- Ototoxicity, Nephrotoxicity.
Rx : Amphostine , Saline. - Busulfan : S/E- Pulmonary Fibrosis
- Cyclophosphamide: Guanine liver bioactivation
S/E: Hemorrhagic Cystitis , SIADH
Rx: Mesna - Carmustine: Crosses BBB, Brain bioactivation
S/E : CNS toxicity
Anti Cancer Drugs
S-Phase Inhibitors
- S-phase synthesizes DNA
- Cladribine: Purine analog,
S/E; Neuro/Nephrotoxicity. - Cytarabine: Pyrimidine analog
S/E: Pancytopenia. - 5-FU : Pyrimidine analog
Inhibits Thymidyl Synthase
S/E: Hand foot syndrome - Methotrexate : Inhibits dihydrofolate reductase
S/E: Myelosuppression
Rx : Leucovorin - Other s-phase inhibitors like azathioprine, 6-merceptopurine & hydroxyurea have their own cards.
Anti Cancer Drugs
G-2 Phase Inhibitors
- Teniposide & Etoposide :
Inhibits Topoisomerase 2. - Topotecan & Irinotecan :
Inhibits Topoisomerase 1.
Anti Tumor Antibiotics
- Doxorubicin & Danorubicin :
- Intercalates DNA
- S/E: Dilated Cardiomyopathy.
- Rx: Dexarazone
- Bleomycin : Generates Free radicals
- S/E: Pulmonary Fibrosis
OCP Note
OCP are contraindicated in women over 35yrs old who are smokers because of increase risk of thromoboembolitic event (i.e pulmonary embolisim)
Hep-C therapy?
- Ribavirin: Nucleotide synthesis inhibitor.
- Sofosbuvir: RNA-Dependent RNA-polymerase inhibitor.
- Simeprevir: Protease Inhibitor.
- Ledipasvir: NS5A Inhibitor.
Linezolid
- Linezolid blocks bacterial protein synthesis by binding 50S ribosomal subunit.
- It has activity against gram-(positive) bacteria.
Penicillin
- Penicillin inhibits bacterial cell wall synthesis by binding transpeptidase enzyme.
- This primarily prevents (peptidoglycan crosslinking).
Vancomycin
- 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).
Azithromycin, clarithromycin, erythromycin are examples of what class of antibiotics?
- Macrolides
- They inhibit bacterial protein synthesis by binding the 50S ribosomal
subunit.
Ciprofloxacin, levofloxacin, and moxifloxacin are examples of what class of antibiotics?
- Fluoroquinolones
- They block bacterial synthesis of DNA by inhibiting (DNA gyrase [topoisomerase II]) and (topoisomerase IV).
Vancomycin is used for which organism and what is the mechanism for its resistance?
- 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.
Sevelamer
- Sevelamer (a phosphate binder) is used to manage hyperphosphatemia in chronic kidney disease.
Which class of antidiabetic drugs decreases insulin resistance by activating peroxisome proliferator–activated receptor gamma?
Thiazolidinediones (eg, pioglitazone).
Acarbose
- Inhibits (alpha-glucosidase) located in the intestinal brush border. - - This leads to decreased postprandial absorption of glucose.
What is the hematologic adverse effect associated with thionamides (eg, methimazole, propylthiouracil)?
- Drug-induced neutropenia/agranulocytosis.
- Thioamides are used in the treatment of hyperthyroidism.
- Methimazole and propylthiouracil are indicated for the treatment of hyperthyroidism. They inhibit (thyroid peroxidase).
Name 2 classes of antidiabetic drugs that inhibit the potassium channel on the pancreatic beta cell membrane:
- Sulfonylureas (eg, glyburide, glipizide)
- Meglitinides (eg, repaglinide)
They induce insulin release independent of blood glucose concentrations, which increases the risk of (hypoglycemia).
Antidiabetic drug that decreases hepatic gluconeogenesis by inhibiting mitochondrial glycerophosphate dehydrogenase?
- Metformin (reduces the availability of substrates for gluconeogenesis)
- This drug has a (low) risk of hypoglycemia (because it does not increase endogenous insulin secretion).
What is the mechanism of action of the following anesthetics?
- Lidocaine: Blocks voltage gated Na channels
- Propofol: Potentiates GABA A receptor
- Ketamine: Inhibits NMDA receptors
Denosumab
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.
Cisplatin
- Cross-links DNA to inhibit DNA synthesis
Toxicity:
- Nephrotoxicity
- Ototoxicity
- Peripheral neuropathy
Cyclophosphamide
- Cross-links DNA to inhibit DNA synthesis
Toxicity:
- Hemorrhagic cystitis
- Bladder cancer
Paclitaxel
- Inhibits microtubule disassembly
- Toxicity: Neuropathy
Vincristine/vinblastine
- Binds β-tubulin to inhibit microtubule formation
- Toxicity: Neuropathy
Anthracyclines (eg, doxorubicin)
- Binds with topoisomerase II to cleave DNA
- Binds with iron to generate free radicals
- Toxicity: Dilated cardiomyopathy
Bleomycin
- Induces free radical formation
- Toxicity: Pulmonary fibrosis
