Unit one pharm flashcards

pharmaceutics

• The study of how various drug forms influence the way in which the drug affects the body 

• Dissolution– dissolving of solid dosage forms and their absorption 

• Different drug dosage forms have different pharmaceutical properties 

• Dosage form determines drug dissolution rate 

Pharmacokinetics

The study of what the body does to the drug

absorption, distribution, metabolism, excretion

absorption (first pass effect)

• Bioavailability: The extent of drug absorption 

• First pass effect: a large proportion of a drug is chemically changed into inactive metabolites by the liver. much smaller amount will be bioavailable-

• if high first pass more drug needs to be given

distribution

• Transport of a drug by the bloodstream to its site of action 

• Albumin is the most common blood protein and carries the majority of protein-bound drug molecules

• -if pt is protein malnourished albumin is low. Medications will not work well if they are highly protein bound

metabolism

• Also referred to as biotransformation 

• Biochemical alteration of a drug into an inactive metabolite, a more soluble compound, a more potent active metabolite (as in the conversion of an inactive prodrug to its active form), or a less active metabolite

• Cytochrome P-450 enzymes (or simple P-450 enzymes), also known as microsomal enzymes

• Lipophilic: fat-loving 

• hydrophilic: water-loving 

• Enzymes 

• Prodrugs 

Cytochrome P-450 enzymes

 found primarily in liver; heme-containing proteins, crucial for metabolizing drugs, toxins, and other compounds by making them more water soluble for excretions

lipophilic

 “fat loving” better for older adults

hydrophilic

“water loving” pts have to be well hydrated or it won’t work

-better for infants

enzymes

 catalysts that break things down

prodrugs

inactive drug molecules transformed into active agents with enzymatic and chemical processes

Excretion

• Elimination of drugs from the body 

• Renal excretion (primary organ responsible for excretion) 

• Biliary excretion 

• Bowel excretion  

• half life

• steady state

• peak level

half-life

time required for half 50% of a given drug to be removed from the body

-after approximately 5 half-lives most dugs are considered to be effectively removed from the body

  -steady state:

physiologic state in which the amount of drug removed via elimination is equal to amount of drug absorbed with each dose

peak level

     -maximum amount of drug in the body

-if peak level too high drug toxicity may occur

Pharmacodynamics

• The study of what the drug does to the body 

1. Drug-receptor relationships 

2. The mechanism of drug actions in living tissues 

3. Therapeutic effect 

4. Enzymes 

5. Nonselective interactions

pharmacogenomics

 study of the economic factors influencing the cost of drug therapy

          -cost-benefit analysis

Pharmacotherapeutics

 the clinical use of drugs to prevent and treat diseases

-defines principles of drug actions, and the cellular processes that change in response to the presence of drug molecules

-drugs are organized into pharmacologic classes

Pharmacognosy

• The study of natural (versus synthetic) drug sources (i.e., plant, animals, minerals) 

toxicology

• Science of the adverse effects of drugs and other chemicals on living organisms 

half-life

• Time required for half (50%) of a given drug to be removed from the body 

• Measures the rate at which the drug is eliminated from the body 

• After approximately five half-lives, most drugs are considered to be effectively removed from the body

steady state

physiologic state in which the amount of drug removed via elimination is equal to the amount of drug absorbed with each dose

peak level

• The length of time for the onset, peak of action, and the duration of action play an important part in determining the peak level (highest blood level) and trough level (lowest blood level) of a drug 

• The highest blood level of a drug

trough level

• The length of time for the onset, peak of action, and the duration of action play an important part in determining the peak level (highest blood level) and trough level (lowest blood level) of a drug 

• The lowest blood level of a drug

toxicity

• If the peak blood level is too high, then drug toxicity may occur 

• Occurs if the peak blood level of the drug is too high 

• Therapeutic drug monitoring

tolerance

Decreasing response to repeated drug doses

dependence

Physiologic or psychological need for a drug

Physical Dependence

Physiologic need for a drug to avoid physical withdrawal symptoms

Psychological Dependence

Also known as addiction and is the obsessive desire for the euphoric effects of a drug

Adverse drug reactions

drug interactions / adverse drug reaction

drug interaction

1. Additive effects

2. Synergistic effects  

3. Antagonistic effects

4. Incompatibility

Additive effects

(1+1=2)

Ex: double caffeine = super energized

Synergistic effects

(1+1>2)

 inhaler plus albuterol better that 2 inhalers

Antagonistic effects

(1+1<2)

opioid and Narcan

Incompatibility:

often IV meds- can two different IV meds be given together at the same time

adverse drug event

1. Medication error 

2. Adverse drug reaction

Drug effects

• Pharmacologic reaction 

• Hypersensitiviy (allergic) reaction 

• Idiosyncratic reaction 

• Drug interaction

• Other drug effects: 

1. Teratogenic 

2. Mutagenic 

3. Carcinogenic effects

teratogenic

babies affected

Mutagenic

gene mutations

Carcinogenic effects

cause cancer

clonidine

• Used primarily for its ability to decrease blood pressure 

• Also used for management of opioid withdrawal 

• Oral and topical patch 

• Do not stop abruptly could cause withdrawal

1. May lead to rebound hypertension

losartan classifiation

• ARB

• ARBs affect primarily vascular smooth muscle and the adrenal gland 

• Selectively block the binding of All to the type 1 All receptors in these tissues 

• ARBs block vasoconstriction and the secretion of aldosterone 

• ARBs do not cause a dry cough 

losartan indication

1. Hypertension

2. Adjunctive drugs for the treatment of HF 

3. May be used alone or with other drugs such as diuretics

losartan side effects

1. Chest pain 

2. Fatigue 

3. Hypoglycemia 

4. Diarrhea

5. Urinary tract infection 

6. Anemia (monitor CBC and iron) 

7. Weakness 

8. Hyperkalemia and cough are less likely to occur than with the ACE inhibitors 

losartan contraindicated

•  patients with renal or hepatic dysfunction and in patients with renal artery stenosis 

• Not safe for breastfeeding women and should not be used in pregnancy 

hydralazine classification

Vasodilator: directly relax arteriolar or venous smooth muscle that results in decreased SVR, decreased afterload, and peripheral vasodilation

hydralazine indications

1. Hypertension 

2. May be combined with other drugs

hydralazine side effects

1. Dizziness 

2. Headaches 

3. Anxiety

4. Tachycardia 

5. Edema 

6. Dyspnea 

7. Nausea 

8. Vomiting 

9. Diarrhea 

10. Hepatitis 

11. Systemic lupus 

12. Erythematosus 

13. Vitamin B6 deficiency 

14. Rash

hydralazine injection methods and why

• Orally: routine cases of essential hypertension 

• Injectable: hypertensive emergencies (or people who can’t do it orally) 

• BiDil: specifically indicated as an adjunct for treatment of HF in African-American patients

hydralazine contraindications

1. Drug allergy

2. Coronary artery disease

3. Mitral valve dysfunction

Bidil

• A combination drug product is available as a tablet containing:

1. Hydralazine 37.5 mg

2. Isosorbide dinitrate 20 mg (an antianginal drug)

• The hydralazine–isosorbide dinitrate combination has been shown to:

1. Improve patient survival

2. Prolong time to hospitalization for heart failure

nitropress classification

Vasodilator: directly relaxes arteriolar or venous smooth muscle, resulting in decreased SVR, decreased afterload, and peripheral vasodilation

nitropress indications

• Used for a hypertensive emergency 

• Sodium nitroprusside and IV diaoxide are reserved for the management of hypertensive emergencies

nitropress side effects

1. Bradycardia 

2. Decreased platelet aggregation 

3. Rash 

4. Hypothyroidism 

5. Hypotension 

6. Methemoglobinemia 

7. Cyanide toxicity

nitropress contradictions

• Used in the intensive care setting for severe hypertension emergencies: titrated to effect by IV infusion 

• Contradictions: 

1. Known hypersensitivity to the drug 

2. Severe HF 

3. Inadequate cerebral perfusion

metoprolol classification

Beta Blocker

Reduction of the heart rate through beta 1 receptor blockage

metoprolol used for

• Decreases myocardial contractility, helping to conserve energy or decrease demand 

• Slow the heart rate

• Long-term use causes reduced peripheral vascular resistance

• treat angina

metoprolol indication

1. Angina 

2. MI 

3. Hypertension 

4. Dysrhythmias

metoprolol contraindications

1. Systolic HF 

2. Serious conduction disturbances

norvasc

• Calcium channel blockers

• Prevent muscle contraction resulting in decreased peripheral smooth muscle tone, decreased SVR, and decreased BP

norvasc indications

1. Angina 

2. Hypertension

3. Dysrhythmias 

4. Migraine headaches 

5. Raynauds disease 

6. Prevent the cerebral artery spasms after subarachnoid hemorrhage: nimodipine

atorvastatin

• HMG-CoA reductase inhibitors (statins) 

• Lower the rate of cholesterol production 

• One of the most commonly used drugs in this class of cholesterol-lowering drugs 

• Lowers total and LDL cholesterol levels as well as triglyceride levels and raises “good” cholesterol, the HDL component 

• Dosed once daily, usually with the evening meal or at bedtime to correlate with diurnal rhythm

atorvastatin indication

1. First-line drug therapy for hypercholesterolemia 

2. Treatment of types lla and llb hyperlipidemias 

3. reduces LDL levels by up to 50% 

4. Increased HDL levels by 2% to 15% 

5. Reduces triglycerides by 10% to 30% 

6. Reduces CVD risk

atorvastatin adverse effects

1. mild , transient gastrointestinal (GI) disturbances 

2. Rash 

3. Headache

4. Myopathy (muscle pain) possibly leading o the serious condition rhabdomyolysis 

5. Elevations in liver enzymes or liver disease 

• NO GRAPEFRUIT

Niacin

• Vitamin B3 

• Lipid-lowering properties require much higher doses than when used as a vitamin 

• effective, inexpensive, often used in combination with other lipid-lowering drugs 

• Not a first line drug 

• Thought to increase the activity of lipase, which breaks down lipids 

• Reduces the metabolism or catabolism of cholesterol and triglycerides 

niacin indications

1. Effective in lowering triglyceride, total serum cholesterol and LDL levels 

2. Increases HDL levels 

3. Effective in the treatment of types lla, llb, lll, IV, and V hyperlipidemias

niacin adverse effects

1. Flushing (caused by histamine release): a small dose aspirin or NSAIDS 30 minutes before Nician may help reduce flushing

2. Pruritis 

3. GI distress 

• Start on a low dose and take before meals

niacin contraindications

• Niacin is contraindicated in patients with:

  • Known hypersensitivity to niacin

  • Liver (hepatic) disease

  • Peptic ulcer disease

  • Active hemorrhage

  • Gout

• Niacin is also contraindicated in:

  • Lactating women

garlic

• Used as an antipasmodic, antihypertensive, antiplatelet, and lipid reducer 

• Adverse effects: dermatitis, vomiting, diarrhea, and flatulence. Antiplatelet activity

• Possible interactions with warfin adn diazepam 

• May enhance bleeding when taken with nonsteroidal anti-inflammatories

• Thins the blood

flax

• Both the seed and oil of the plant are used 

• Uses; atheroscleroiss, hypercholesterolemia, GI distress, menopausal symptoms 

• May cause diarrhea and allergic reactions 

• Possible interactions: antidiabetic drugs, anticoagulant drugs

nitrate

• Causes vasodilation because of relaxation of smooth muscles: potent dilating effect onthe  coronary arteries 

• Result: oxygen to ischemic myocardial tissue

• High first pass effect. Some routes bypass the first pass effect, so we have to give less (sublingual, IV, Transdermal patches, and transdermal sprays) 

nitrate indication

(for chest pain)

1. Treat stable, unstable, and vasospastic angina 

2. Rapid-acting forms (treat acute anginal attack, sublingual tablets, and IV infusion) 

3. Long-acting forms (used to prevent anginal episodes) 

nitrate available forms

1. Sublingua; chewable tablets 

2. Oral capsules/tablets 

3. Intravenous solution 

4. Transdermal patches 

5. Ointments 

6. Translingual sprays

nitrate types

1. Nitroglycerin ( both rapid and long acting) 

2. Isosorbide dinitrate (both rapid and long acting)

3. Isosorbide mononitrate (primarily long-acting)

nitrate contradictions

1. Known drug allergy 

2. Severe anemia 

3. Closed-angle glaucoma 

4. Hypotension (because it is going to lower their BP even more) 

5. Severe had injury 

6. Use of the erectile dysfunction drugs sildenafil, tadalafil, and vardenafil

nitrate adverse effects

1. Headaches 

• Usually diminish in intensity and frequency with continued use

• Do not touch a nitrate with an ungloved hand 

• Touching a nitro will give you an awful headache 

2. Reflex tachycardia 

3. Postural hypotension 

4. Skin irritation with topical application 

• Not always a true allergy 

5. Tolerance may develop 

nitrate and tolerance

1. Prevented by allowing a regular nitrate-free period, allowing enzyme pathways to replenish 

2. Remove the patch for 8 hours to prevent tolerance 

3. You may have to have an increasing dose to have the same effect

Isosorbide Dinitrate

• Organic nitrate 

• Available in rapid-acting sublingual tablets, immediate-release tablets, long acting oral dosage forms 

• Produces more consistent, steady, therapeutic response

lisinopril

• ACE inhibitors

• Often used as first-line drugs for HF and hypertension 

• May be combined with a thiazide diuretic or CCB 

lisinopril and diabetes

Cardiovascular drugs of choice for patients with diabetes (standard therapy for diabetic patients to prevent the progression of diabetic nephropathy) (renal protectives)

lisinopril how it works

• Affects the cardiovascular and renal systems 

• Reduces BP by decreasing SVR (preload) 

• Decreases workload on the heart to affect HF (prevents sodium and water reabsorption, so it is excreted through the urine) 

lisinopril and MI

• Used to prevent complications after MI 

• Reduces ventricular remodeling (left ventricular hypertrophy, which is sometimes seen in MI) 

lisinopril adverse effects

1. Fatigue 

2. Dizziness

3. Headache

4. Mood changes (it has a depressive effect) 

5. Impaired taste 

6. Possible hyperkalemia 

7. Dry mouth, nonproductive cough. Which reverses when therapy is stopped 

8. Angioedema: rare but potentially fatal

MAJOR lisinopril symptom

dry cough

digoxin

is a cardiac glycoside used to treat heart failure and atrial fibrillation by strengthening heart contractions and slowing heart rate.

Digoxin (Lanoxin) is indicated for the treatment of:

1. Heart failure

2. Atrial fibrillation

3. Atrial flutter

Contraindications to digoxin use include:

1. Known hypersensitivity to digoxin

2. Ventricular tachycardia

3. Ventricular fibrillation

Therapeutic serum digoxin levels:

1. Normal range: 0.5–2 ng/mL

2. Levels greater than 2 ng/mL may be used for the treatment of atrial fibrillation

Digoxin is available in:

1. Oral formulations

2. Injectable formulations

Digoxin fab (digibind) therapy

digoxin toxicity antidote

• Hyperkalemia (serum potassium greated than 5 mEq/L) in digitalis-toic patient 

• Life threatening cardiac dysrhythmias 

• Life threatening digoxin overdose

Conditions that predispose to digoxin toxicity

1. Hypokalemia 

2. Use of cardiac pacemaker 

3. Hepatic dysfunction 

4. Hypercalemia 

5. Dysrythmais 

6. Hypothyroid, respiratory, or renal disease 

7. Advanced age

Amiodarone

• Class III

• Temporary control of a rapid ventricular response in patients with atrial fibrillation or flutter and PSVT

amiodarone contradictions

 hypersensitivity, acute myocardial infarction, pulmonary congestion, Wolff-Parkinson-White syndrome, severe hypotension, cardiogenic shock, sick sinus syndrome, or second- or third-degree AV block

Amiodarone (Cordarone, Pacerone) 

• Markedly prolongs:

• Action potential duration

• Effective refractory period in all cardiac tissues

Amiodarone Blocks both:

• Alpha-adrenergic receptors

• Beta-adrenergic receptors of the sympathetic nervous system

One of the most effective antidysrhythmic drugs for

• Supraventricular dysrhythmias

• Ventricular dysrhythmias

antidysrhythmic Indicated for management of:

• Sustained ventricular tachycardia (VT)

• Ventricular fibrillation (VF)

• Nonsustained VT

Amiodarone Pharmacokinetics and Chemical Properties

• Amiodarone is highly lipophilic (fat-loving):

  • Penetrates and concentrates in adipose tissue of multiple organs

• Contains iodine in its chemical structure

• The thyroid gland sequesters iodine, leading to potential thyroid effects:

  • Hypothyroidism

  • Hyperthyroidism

Amiodarone Adverse Effects (General)

• Adverse reactions occur in ~75% of patients

• Incidence and severity are higher with:

  • High doses (>400 mg/day)

  • Prolonged therapy

Amiodarone Common Adverse Effects

• Corneal microdeposits (very common):

  • Occur in virtually all adults taking the drug >6 months

  • May cause:

    • Visual halos

    • Photophobia

    • Dry eyes

• Photosensitivity:

  • Occurs in 10%–75% of patients

Amiodarone Serious Adverse Effects and Black Box Warning

• Pulmonary toxicity (most serious):

  • Fatal in approximately 10% of patients

  • Symptoms include:

    • Progressive dyspnea

    • Cough

  • Can result in pulmonary fibrosis

• Proarrhythmic effects:

  • Amiodarone may provoke dysrhythmias while treating them

• Black box warning includes risk of:

  • Hepatotoxicity

  • Pulmonary toxicity

  • Proarrhythmic effects