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AANP/ANCC > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Pharmacokinetics

A

Study of how drugs move throughout the body; includes absorption, distribution, metabolism and elimination.

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2
Q

Pharmacodynamics

A

Study of what a drug does to the body; generally determined by the drug’s affinity and activity at its site of action, which often times is a receptor

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3
Q

Bioavailability

A

Ability of a drug to be absorbed and used by the body

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4
Q

Half-life

A

The time it takes for the amount of a drug’s active substance in the body to reduce by half

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5
Q

Drug metabolism - First pass effect

A

Pharmacological phenomenon in which a drug undergoes metabolism at a specific location in the body thereby reducing the availability of the drug to travel to distant sites.

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6
Q

Drug metabolism - Cytochrome P450 system

A

Group of enzymes that metabolizes drugs; largely concentrated in the liver.

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7
Q

Strong inhibitor drugs

A

Clarithromycin
Darunavir
Ketoconazole
Lopinavir
Nirmatrelvir-ritonavir
Saquinavir
Voriconazole

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8
Q

Moderate Inhibitor drugs

A

Amiodarone
Cimetidine
Cyclosporine
Diltiazem
Erythromycin
Fluconazole
Grape fruit juice
Letermovir
Verapamil

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9
Q

Strong Inducer drugs

A

Apalutamide
Carbamazepine
Encorafenib
Fosphenytoin
Lumacaftor-ivacaftor
Mitotane
Phenobarbital
Primidone
Rifampin

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10
Q

Moderate Inducer drugs

A

Bexarotene
Cenobomate
Dexamethasone
Eslicarbazepine
Mitapivat
Modafinil
Pexidartinib
Rifabutin
St. John’s Wort

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11
Q

Drug Elimination - Glomerular Filtration

A

Works to filter waste and excess fluid from the blood into the urine

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12
Q

Drug elimination - Glomerular Barrier

A

Restricts passage of plasma proteins, such as albumin, red blood cells, and o their large blood constituents.

Drugs that bind to albumins, barbiturates, benzodiazepines penicillin, valproate, phenytoin, warfarin and NSAIDs

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13
Q

Drug Elimination - Renal excretion and aging

A

Glomerular filtration rate decreases by approximately 1% per year.

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14
Q

Non-steroidal Anti-Inflammatory Drugs (NSAIDs)

A

Primary effect of NSAIDs is to inhibit cyclooxygenase (an enzyme that produces prostaglandins)

Prostaglandins: hormone-like substances that affect several bodily functions (Inflammation, pain)

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15
Q

Two Variants of Cyclooxygenase

A

COX 1: Helps to regulate normal cellular functions (Vascular homestasis, platelet aggregation, kidney function)
- Aspirin inhibits platelet aggregation associated with COX-1 in an irreversible manner.

COX 2: Expressed in the brain, kidney, bone and likely the female reproductive system
- COX-2’s expression is increased during states of inflammation and is inhibited by glucocorticoids

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16
Q

Medications to avoid with NSAIDs

A

Phenytoin
Warfarin
Methotrexate
ACE Inhibitors
Glucocorticoids

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17
Q

Population that should avoid NSAIDs

A

Peptic ulcer disease
Gastrointestinal disease
Cardiovascular disease
Kidney disease

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18
Q

Gram stain

A

Categorizes bacteria into either gram-negative or gram-positive bacteria

  • Gram-positive bacteria: Retain the violet and appear purple with gram staining
  • Gram-negative bacteria: take up the safranin counterstain and appear pink
  • Gram variable: Meaning they may stain either negative or positive (Example: Gardnerella Vaginalis)

CAN NOT BE VISUALIZED BY GRAM STAIN
- Mycoplasma species: lacks a cell wall
- Chlamydia and Mycobacterium: Cell wall structure does not retain gram stain reagents.

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19
Q

Gram-Positive Bacteria

A

Streptococcus
Staphylococcus
Enterococcus
Clostridium Difficle
Listeriosis
Diptheria
Botulism
Tetanus
Anthrax

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20
Q

Gram-Negative Bacteria

A

Neisseria Meningitidis or Neisseria Gonorrhoeae
Moraxella Catarrhalis
Escherichia
Klebsiella
Enterobacter
Pseudomonas
Haemophilus
Acinetobacter
Moraxella
Prevotella
Porphyromonas

21
Q

Beta Lactam antibiotics

A

Includes Penicillins and cephalosporins (Both contain beta lactam ring in their chemical make up)
- Resistance due to beta lactamase
- Clavulanic acid protects against beta lactamase

22
Q

Penicillin G

A

Active against: Gram positive cocci, gram positive rods (listeria), gram negative cocci (neisseria), most anaerobes, spirochetes

23
Q

Anti-Staphylococcal Penicillins

A

Nafcillin, Oxacillin, Dicloxacillin

Active against: Penicillinase-producing staphylococci, staphylococcus aureus

24
Q

Broad spectrum penicillins

A

Second generation: Ampicillin, Amoxicillin

Active against: Gram-negative bacilli, the majority of strains of Escherichia coli, Proteus mirabilis, Salmonella, Shigella, and Haemophilus Influenzae

  • Generally PO Amoxicillin is preferred over ampicillin
    • Ampicillin is preferred for the treatment of shigella

Third generation: Ticarcillin

Fourth Generation: Piperacillin
- Broad spectrum agents are active against gram-negative bacilli

25
Cephalosporins - First Generation
Cephalexin Active against: Most gram-positive cocci, most strains of Escherichia coli, proteus mirabilis, and klebsiella pneumoniae
26
Cephalosporins - Second Generation
Cefuroxime, Cefaclor, Cefprozil Active against: Haemophilus Influenzae, Moraxella Catarrhalis
27
Cephalosporins - Third Generation
Ceftibuten, Cefixime Active against: Enterobacterales, Neisseria, H. Influenzae
28
Cephalosporins - Fourth Generation
Cefepime Active against: Enterobacterales, Neisseria, H. Influenzae, P. Aeruginosa
29
Cephalosporins - Fifth Generation
Ceftaroline Active against: Methicillin-resistant staphylococci, Penicillin-resistant pneumococci, enteric gram-negative rods.
30
Tetracyclines
Doxycycline, Minocycline Active against: Many aerobic gram-positive and gram-negative bacteria and atypical pathogens such as mycoplasma and chlamydia - Associated with permanent tooth discoloration in children < 8 years of age and with accumulating in fetal bones and teeth if it’s administered to pregnant women. - First line treatment for chlamydia and the prophylaxis/treatment of Lyme disease - Avoid concurrent use with penicillins
31
Sulfonamides
Trimethoprim/Sulfamethoxazole (Bactrim) Active against: Variety of aerobic gram-positive and gram-negative bacteria, methicillin-resistant staphylococcus aureus
32
Fluroquinolones
Ciprofloxacin, Levofloxacin Active against: Aerobic enteric gram-negative bacilli, many common respiratory pathogens, Pseudomonas selected gram-positive organisms, anaerobes, mycobacteria, tuberculosis, anthrax - Ciprofloxacin: Activity against aerobic enteric gram-negative bacilli (Example: E. Coli), Pseudomonasaeruginosa - Levofloxacin: Activity against gram-positive organism (Example: Streptococcus pneumoniae and staphylococcus aureus) Potential adverse effects with fluroquinolones: C. Diff infection, tendinopathy, tendon rupture, neuropathy, QT Interval prolongation, small alleged risk of aortic dissection and rupture.
33
Beta Blockers
They block beta adrenergic receptors - Beta-1: Found mainly in the heart and kidneys - Beta-2: Found mainly in smooth muscle tissue, within the respiratory system, blood vessels and nervous system - Beta-3: Found mainly in fat cells and within the bladder
34
Cardioselective Beta Blockers (B1 receptor)
Acebutolol Atenolol Betaxolol Bisoprolol Esmolol Metoprolol Nebivolol
35
Non-selective beta blockers
Carvediolol Labetolol Nadolol Penbutolol Propranolol Sotalol Timolol
36
Angiotensin Converting Enzyme Inhibitors (ACEI)
- Prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor - First line treatment for hypertension - Preferred option in patients with chronic kidney disease, and heart failure Examples: Lisinopril, Benazepril, Captopril, Enalapril Side effects: Related to either decreased angiotensin II or increased kinins - Decreased angiotensin II: - Hypotension, acute kidney injury, hyperkalemia and pregnancy complications - If hyperkalemia occurs and is unable to be managed or if creatinine increases > 30% baseline within the first 6 - 8 weeks, ACE termination should be considered. - Increased Kinins: - Dry hacking cough, angioedema (rare but life threatening) IMPORTANT POINTS - Contraindicated in pregnancy - ACE Inhibitors and ARBs CAN NOT be taken together.
37
Calcium Channel Blockers
- First line treatment for hypertension - Can be used as monotherapy or adjunct treatment - Significant amount of data supporting CCBs reduction in subsequent cardiac events - Metabolized through the cytochrome P450 system
38
Calcium Channel Blockers - Non-Dihydropyridines
- Weaker vasodilator, works more to decrease the contractility of the heart - Used for hypertension (not often), chronic stable angina, cardiac arrhythmias EXAMPLES: Verapamil & Diltiazem Side effects: Constipation, bradycardia, decreased cardiac output, gingival hyperplasia
39
Calcium Channel Blockers - Dihydropyridines
- Potent vasodilators with minimal cardiac effects - Used for hypertension or chronic stable angina EXAMPLES: Amlodipine, Nifedipine, Nicardipine Side effects: Headache, lightheadedness, flushing, dependent peripheral edema, gingival hyperplasia - Treat peripheral edema by reducing CCB dose, switch to a non-dihydropyridine and/or add a RAS-blocking agent (ACE or ARB)
40
Statins
Statin therapy is first line treatment for dyslipidemia 3-types: Low intensity, moderate intensity, and high intensity.
41
Low intensity Statin
Lovastatin (20mg) Pravastatin (10-20mg) Simvastatin (10mg) Fluvastatin (20-40mg)
42
Moderate intensity Statin
Lovastatin (40-80mg) Pravastatin (40-80mg) Simvastatin (20-40mg) Atorvastatin (10-20mg) Rosuvastatin (5-10mg)
43
High intensity Statin
Atorvastatin (40-80mg) Rosuvastatin (20-40mg)
44
BEFORE initiating Statin therapy
Get baseline aminotransferase levels - In the presence of liver disease - Pravastatin and Rosuvastatin are preferred - Alcohol abstinence is imperative - Start at a very low statin dose and titrate based on aminotransferase levels - Re-evaluate in 4-12 weeks and re-check aminotransferase levels - Checkk thyroid function (TSH) - Hypothyroidism is a potential cause for dyslipidemia and can make patients more susceptible to muscle injury
45
Muscle injury associated with Statin use
Risk is highest with statins extensively metabolized by the Cytochrome P450 3A4 - Examples: Lovastatin, Simvastatin, Atorvastatin IF muscle injury occurs: - STOP statin - Evaluate potential contributing factors - Hypothyroidism - Vitamin D deficient - Medicate interactions - Treatment options - Restart at lower dose - Switch statin agent - Attempt alternate day dosing - Switch to non-statin cholesterol lowering agent.
46
Digoxin
- Cardiac glycoside that is used for heart failure and supraventricular arrhythmias - Inhibits the sodium potassium pump, which causes a temporary increase in intracellular sodium, causing calcium to influx through the sodium calcium exchange pump, leading to increased contractility. - Narrow therapeutic index - Heart failure: The therapeutic serum concentration is 0.5-0.9 ng/mL - Atrial Fibrillation: The therapeutic serum concentration is 0.8-2 ng/mL Digoxin Toxicity: Arrhythmias, gastrointestinal symptoms, confusion and vision changes (Halos or xanthopsia)
47
Levothyroxine
- Synthetic T4 - First line treatment for hypothyroidism - Levothyroxine’s onset of action when taken orally is 3-5 days but does not reach its peak therapeutic effect until 4-6 weeks later DOSING Being at full dose UNLESS - Patients with cardiac history and > 60 years on low dose (25-50 mcg/day) - Re-check TSH in 4-6 weeks and titrate dose if needed slowly - Take on empty stomach
48
Metformin
- First line treatment for Type 2 Diabetes Decreases hepatic glucose by inhibiting gluconeogensis, decreases intestinal absorption of glucose and improves insulin sensitivity. Benefits: - Decreases A1C by 1-2%, not known to cause hypoglycemia, has shown to decrease food intake and body weight and may help reduce likelihood of cardiac events Side effects: - Diarrhea! - Stop and wait for diarrhea to resolve before attempting metformin again at a lower dose and slowly titrate to desired dose. Contraindications: - Hypersensivitiy to metformin or any component of the formulation: severe renal dysfunction (eGFR <30), acute or chronic metabolic acidosis with or without coma. Risk factors for lactic acidosis: - Impaired kidney function (eGFR <30) - Active liver disease - Metabolic acidosis - Dehydration - Sepsis - History of lactic acidosis
49
Selective Serotonin Reuptake Inhibitors (SSRI)
First line treatment for unipolar depression - Also used for anxiety disorders eating disorders, obsessive-compulsive disorders and PTSD. SSRIs work by blocking the reabsorption of serotonin, allowing more serotonin to be available. EXAMPLES: Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Citalopram (Celexa), and Escitalopram (Lexapro) Side effects: GI Discomfort (Diarrhea), sexual dysfunction and weight gain IMPORTANT POINTS - Start at sub therapeutic dose and titrate up - Screen the patient for bipolar disorder before beginning SSRI - IF SSRI is stopped, taper is slowly.

AANP/ANCC (17 decks)

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