Pharmacology Flashcards
Natural PCNs (Drugs)
Penicillin G
Penicillin V
Natural PCNs (Spectrum)
Gram +, cocci and bacilli, some gram -
Penicillinase resistant PCN (Drugs)
Nafcillin, methacillin, cloxacillin, dicloxacillin, oxacillin
Penicillinase resistant PCN (Spectrum)
Staph. Aureus
Extended spectrum (Drugs)
Ampicillins, amoxicillin, bacampicillin
Extended spectrum (Spectrum)
Gram +/-, cocci and bacilli
Antipseudomonals (Drugs)
Ticarcillin, piperacillin, carbenicillin, mezlocillin
Antipseudomonals (Spectrum)
Gram (-) plus pseudomonas
Penicillin/Beta lactamase inhibitors (Drugs)
amoxicillin clavulanate (Augementin)
ampicillin/sulbactam (Unasyn)
piperacillin/tazobactam (Zosyn)
ticarcillin/clavulanate (Timentin)
1st generation cephalosporins (drugs)
“Cefa” “Cepha” “Cephra”
Except Cefaclor which is 2nd gen
2nd generation cephalosporins (drugs)
Cefuroxime, Cefoxitin, Cefotetan, Cefaclor
3rd generation cephalosporins (drugs)
“ime” “one” “ten”
Cefdinir
Moxalactam
Except Cefuroxime which is 2nd gen
4th generation cephalosporins (drugs)
“pi”
Cefepime, Cefepirole
5th generation cephalosporins (drugs)
“rol”
Ceftaroline
1st generation (spectrum)
Gram +, Ok Gram -, anaerobes +/- (not B. fragilis)
2nd generation (spectrum)
Gram +, Good Gram -, anaerobes +/-
3rd generation (spectrum)
Weak Gram +, Better Gram -, anaerobes +/-, ceftazidime active against pseudomonas
4th generation (spectrum)
Gram +, Best Gram -, anaerobes +/-, pseudomonas
5th generation (spectrum)
Gram +, Gram -, anaerobes +/-, MRSA
1st generation (Role)
- S. aureus infections
- Skin, soft tissue infections
- Preoperative antibiotic prophylaxis for clean procedures
- Uncomplicated, community acquired UTIs
2nd generation (Role)
- Surgical prophylaxis in GI surgery
- PID
- Community-acquired pneumonia
- Otitis media
- Sinusitis
- Quinolone, TMP/SMX-resistant E. coli UTI
3rd generation (Role)
- Predominantly GRAM NEGATIVE AGENT
- Community acquired pneumonia
- ECF-acquired pneumonia where Pseudomonas is not suspected
- UTIs with gram (-)
- Meningitis
- Gonorrhea
CEFTAZIDIME = ANTIPSEUDOMONAL
4th generation (Role)
Overly broad
5th generation (Role)
MRSA pneumonia?
Community acquired pneumonia (CAP)
Cellulitis with CANVAS 1 in CANVAS 2
Procaine Pencillin
Formulation of Penicillin G
- Delays peak serum and last 12 hours in serum and tissue
- Common allergy to procaine (injection anesthetic)
Benzathine Penicillin
Formulation of Penicillin G
- Drug of choice for latent syphilis
- Provides long lasting serum levels (15-30 days)
- Not effective against CNS infections
Ampicillin-sulbactam
Common name: Unasyn
Penicillin with Beta-lactamase
Amoxicillin-clavulanate
Common name: Augmentin
Penicillin with Beta-lactamase
Unasyn/Augmentin (spectrum)
Gram +: MSSA
Gram -
Anaerobes: B. fragilis
Unasyn/Augmentin (Role)
- Pneumonia
- Intraabdominal infections
- Skin and soft tissue infections
Piperacillin-Tazobactam
Common name: Zosyn
Penicillin with beta-lactamase
Piperacillin-Tazobactam (Spectrum)
- MSSA
- Beta-lactamase producing Enterobacteriaceae
- B. fragilis
Piperacillin-Tazobactam (Role)
- Nosocomial pneumonia
- Intra-abdominal infections
- Complications infections
- Pseudomonal infections
Cephalosporins (adverse effects)
- Stomach discomfort.
- Nausea or vomiting.
- Diarrhea.
- Thrush (white fungus in the mouth), yeast infection, or other fungal infection.
- Blood abnormalities.
- Rash or itching
Penicillin (adverse effects)
- Oxacillin, nafcillin (Elevated AST/ALT, neutropenia, rash, allergic interstitial nephritis)
- Ampicillin/amoxicillin (Rash, diarrhea)
KPCs
K pneumoniae carbapenemase
Klebsiella and other Enterobacteriaceae produce carbapenemases, which are enzymes that hydrolyze the carbapenems
Aztreonam (Role)
No cross reactivity if patient has a PCN allergy
Gram (-)
Antipseudomonal
Aztreonam (Adverse effects)
Extremely expensive ($150/day)
Imipenem (Adverse effects)
Rapid renal excretion leading to higher incidence of seizures in renal insufficiency patients (A dehydropeptidase inhibitor is added to try to reduce issue)
Imipenem/Meropenem (activity)
Gram +
Gram (-)
Anaerobic activity
Quick resistance from Acinetobacter baumannii
Ceftolozane/Tazobactam (indications)
Use reserved for multi-drug resistant Pseudomonas aeruginosa
Ceftolozane/Tazobactam (disadvantages)
Expensive
Ceftazidime/Avibactam (Indications)
Treatment of carbapenem-resistant Enterobacteriaceae that have Klebsiella producing carbapenemases activity
Ceftazidime/Avibactam (Disadvantages)
Extremely expensive
Hydrocortisone
Common names: Cortenema, Cortifoam
Topical corticosteriod or enema
IBD management
Budesonide
Common names: Uceris, entocort (oral only)
Topical foam or oral corticosteroid
IBD management
Prednisone
Oral corticosteriod
IBD management
Sulfasalazine
Common names: Azulifidine
Class: Aminosalicylate
IBD Management
Mesalamine
Common names:
Canasa (suppository)
Rowasa (enema)
Asacol, apriso, lialda, pentasa, delzicol (oral)
Class: Aminosalicylate
IBD Management
Olsalazine
Common name: Dipentum
Class: Aminosalicylate
IBD management
Balsalazide
Common name: Colazal
Class: Aminosalicylate
IBD management
IBD Management Sequence
Aminosalicylates Corticosteriods Immunomodulators TNF alpha inhibitors Natalizumab Vedolizumad Antibiotics
Immunomodulators for IBD
Azathioprine
Mercaptopurine
Cyclosporine
Methotrexate
Sodium Bicarbonate
Common name: Alka-Seltzer
Antacid
GERD Management
Calcium Carbonate
Common name: Tums
Antacid
GERD Management
Magnesium hydroxide + Aluminum hydroxide
Common name: Mylanta
Antacid
GERD Management
Cimetidine
Common name: Tagamet
H2 Blocker
GERD Management
Famotidine
Common name: Pepcid
H2 Blocker
GERD Management
Ranitidine
Common name: Zantac
H2 Blocker
GERD Management
Nizatidine
Common name: Axid
H2 Blocker
GERD Management
Omeprazole
Common name: Prilosec
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Esomeprazole
Common name: Nexium
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Pantoprazole
Common name: Protonix
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Lansoprazole
Common name: Prevacid
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Dexlansoprazole
Common name: Dexilant
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Rabeprazole
Common name: Aciphex
PPI
GERD Management (1x day) PUD/H. Pylori (Multiple times a day)
Misoprostol
Analogue of PGE, stimulates secretion of mucus and bicarbonate
GERD Management of patients on NSAIDs
Contraindicated in pregnancy
Sucralafate
Salt of sucrose complexed to aluminum hydroxide which forms viscous past that binds selectively on ulcers or erosions
GERD Management
Triple therapy
H. Pylori Management
High dose PPI plus
Antibiotics (Clarithromycin and [Amoxicillin or Metronidazole])
Prevpac
Triple therapy combination product for H. Pylori
Lansoprazole, amoxicillin, clarithromycin
Pylera
Triple therapy combination product for H. Pylori
Bismuth subcitrate potassium, metronidazole, tetracycline
Quadruple Therapy
H. Pylori management
High dose PPI plus
Bismuth subsalicylate plus
Metronidazole and [tetracycline or doxycycline]
Bethanechol
Cholinomimetic agent (stimulates muscarinic receptors and increases smooth muscle tone)
Motility Disorders
Neostigmine
Cholinomimetic agent (Acetylcholinesterase inhibitor and blocks destruction of ACh)
Motility Disorders
Metoclopramide
D2 receptor blocker
Requires renal adjustment
Motility Disorders
Domperidone
D2 receptor blocker
NOT FDA approved
Motility Disorders
Erythromycin
Macrolides (antibiotic)
Motility Disorders
Erythromycin (side effects)
- QTc prolongation, ventricular arrhythmias
- Abdominal pain/cramping, diarrhea
- Decreased efficacy with long term use (4+ weeks)
Erythromycin (Drug interactions)
Numerous, major CYP3A4 inhibitor
Macrolides (MOA)
- Mimics motilin, a potent contractile agent
- Cholinergic facilitation
Domperidone (Side effects)
- QTc prolongation, cardiac arrest
- Abdominal cramps
Domperidone (Drug interactions)
- CYP3A4 inhibitors
- QTc prolonging medications
Metoclopramide (Side effects)
Drowsiness, dystonic reaction, restlessness, bronchospasms, prolactin elevation
Metoclopramide (Drug interactions)
Antipsychotic agents
Atovaquone (antimalarial)
Droperidol
D2 Receptor Blockers (MOA)
Blockade of D2 receptors which leads to increased smooth muscle stimulation
- increased esophageal peristalsis
- increased lower esophageal sphincter pressure
- increased gastric emptying
D2 Receptor Blockers
Common for diabetic gastroparesis
Metoclopramide
Domperidone
Neostigmine (Drug Interactions)
Beta blockers
Corticosteroids
Succinylcholine
Neostigmine (Side Effects)
AV block, bradycardia
Dizziness
Diaphoresis
Bronchospasms
Bethanechol (Side Effects)
Abdominal pain, diarrhea
Urinary urgency
Asthma, bronchoconstriction
Flushing, headache, bradycardia
Bethanechol (Drug interactions)
Acetylcholinesterase inhibitors
Beta blockers
Misoprostol (Side Effects)
Diarrhea, abdominal pain
Detrimental to pregnancy
Misoprostol (Side Effects)
Antacids, magnesium containing
Sucralafate (Side Effects)
Constipation, aluminum toxicity (CKD patients)
Sucralafate (Drug Interactions)
Binds to multiple medications
PPIs (MOA)
Travel systemically to form irreversible disulfide bonds with proton pumps inactiving them
Taken on empty stomach
PPIs (Side Effects)
- Decreased B12, Ca and magnesium absorption
- Increased risk of bone fractures
- Increased risk of C. diff and pneumonia
- Increased risk of dementia and CKD
- Rebound acid hypersecretion with discontinuation
PPIs (Drug Interactions)
Drugs process via CYP2C19
Clopidogrel (Plavix): decreased antiplatelet activity
H2 Blockers (MOA)
Acid inhibition via reversible H2 receptor blockade on parietal cells
H2 Blockers (Side Effects)
Diarrhea, headache, fatigue, constipation, CNS effects (confusion, hallucinations, delirium)
Gynecomastia/impotence (cimetidine only)
H2 Blockers (Drug interactions)
Cimetidine (CYP2C9, CYP2D6, CYP1A2, CYP3A4 inhibitor)
Antacids (MOA)
Neutralize gastric acid by reacting with HCl
Sodium bicarbonate (Side effects)
Belching, metabolic alkalosis, fluid retention
Calcium carbonate (Side effects)
Belching, hypercalcemia, metabolic alkalosis
Magnesium hydroxide + Aluminum hydroxide (Side effects)
Diarrhea, constipation, aluminum accumulation in CKD
Sodium bicarbonate (Drug Interactions)
Elvitegravir (v)
Amphetamines (^)
Calcium-containing dairy products (v)
Calcium carbonate and Magnesium hydroxide + Aluminum hydroxide (Drug interactions)
Tetracyclines (v) Fluoroquinolones (v) Itraconazole (v) Iron (v) Calcium-containing dairy (^) Elvitegravir (v)
Acyclovir (Spectrum)
Anti-viral (15-21% bioavailability)
Herpes simplex (HSV) 1 and 2
Varicella-zoster (VZV)
EBV
Not CMV
Famciclovir (Spectrum)
Anti-viral (77% bioavailability)
Herpes simplex (HSV) 1 and 2
Varicella-zoster (VZV)
EBV
Not CMV
Ganciclovir (Spectrum)
Active against cytomegalovirus (CMV)
Poor bioavailability (5-9%)
Foscarnet (Spectrum)
Anti-viral
GCV resistant CMV,
ACV-resistant HSV 1&2, VZV
Intolerable myelosuppression with GCV
Valacyclovir
Prodrug of Acyclovir combined with valine
Improved bioavailability to 54% but 5x more expensive
Famciclovir
Prodrug of penciclovir
Improved oral bioavailability over ACV of 77%
Oral treatment of VZV
Valaganciclovir
Prodrug, valine ester of Ganciclovir
Improved bioavailability to 60%
Foscarnet (MOA)
Inorganic pyrophosphate analog
Directly inhibits viral DNA polymerase (Reversibly blocks pyrophosphate binding site of viral DNA polymerase)
Renal metabolism
Acyclovir (MOA)
Deoxyguanosine nucleotide analog that inhibits transcription by viral DNA polymerase
Renal metabolism
Ganciclovir (MOA)
Deoxyguanosine nucleotide analog that inhibits transcription by viral DNA polymerase
Renal metabolism
Acyclovir (Toxicity)
Rare, not significant
Nephrotoxicity: can crystallize in renal tubules
Neurotoxicity: lethargy, confusion, delirium
ACV Resistance
Due to loss of viral thymidine kinase, altered TK activity, or DNA polymerase mutants
ACV-R HSV or VSV will be cross-resistant to famciclovir and ganciclovir
Ganciclovir (Toxicity)
Myelosuppression (Neutropenia and thrombocytopenia) CNS toxicity (Headache, change in mental status)
Ganciclovir Resistance
Reduced intracellular phosphorylation due to point mutations/deletions in the UL97 gene
Point mutations in the viral DNA polymerase
Cross resistance to Foscarnet
Foscarnet (Toxicity)
Very significant
Nephrotoxicity (usually 2nd week of therapy)
- Reversible
Metabolic abnormalities
- Hypocalcemia
- Hypomagnesemia
- Hypokalemia
CNS abnormalities
- Headache, irritability, seizures
Painful genital ulcerations
Hep B Therapy Drugs
Lamivudine/emtricitabine (Least potent)
Entecavir
Tenofovir (Most potent)
Hep B Drugs (MOA)
Nuceloside analogs: inhibits hepatitis B DNA polymerase via chain termination
Suppresses replication, not a cure
Interferon alpha 2a or 2b (MOA)
Hep C
Induce interferon-stimulated genes which establish an antiviral state within cells, though the response is not virus specific; inhibit viral protein synthesis
Interferon alpha 2a or 2b (Side effects)
- Fever, myalgia
- Neutropenia, thrombocytopenia
- Hypothyroidism
- Depression
Ribavirin (MOA)
Hep C
Nuceloside analog
Ribavirin (Side effects)
- Hemolytic anemia
- Teratogenic
- Flu-like symptoms
- Depression/irritability
- Rash
- Nausea/diarrhea
Interferon + ribavirin (response rates)
Most responsive to least: 2 and 3 4 5 6 1
Interferon + ribavirin (Limitations)
Not well tolerated
Poor response rates
Long duration of therapy (up to 48 weeks)
Hep C Direct Acting Agents
Protease inhibitors
- Boceprevir
- Telaprevir
- Simeprevir
Only used for Genotype 1
Protease Inhibitors benefits
Increase response rates of Interferon and ribavirin therapy
Decreased length of therapy
Harvoni (MOA)
Sofosbuvir (Nucleoside analog against HCV NS5B polymerase)
Ledipasvir (NS5A inhibitor)
Harvoni (Spectrum)
HCV genotypes 1, 4, 5, and 6
Zapatier (MOA)
Elbasvir (NS5A inhibitor)
Grazoprevir (NS3/NS4A inhibitor)
Zapatier (Spectrum)
HCV Genotypes 1 and 4
Epclusa (MOA)
Sofosbuvir (Nucleoside analog against HCV NS5B polymerase)
Velpatsavir (NS5A inhibitor)
Epclusa (Spectrum)
Pan-Genotypic
HCV Genotypes 1, 2, 3, 4, 5, 6
Mayret (MOA)
Glecabrevir (NS3/4A protease inhibitor)
Pribrentasvir (NS5A inhibitor)
Mayret (Spectrum)
Pan-Genotypic
HCV Genotypes 1, 2, 3, 4, 5, 6