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Pharmacology
Study of drugs and their actions on living organisms
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Pharmacokinetics
concerned with the movement of drugs within the body
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Pharmacodynamics
the branch of pharmacology concerned with the effects of drugs and the mechanism of their action.
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Agonists
a drug attaches to a receptor site and STIMULATES the cell to perform an action
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Antagonists
drug attaches to a receptor site and PREVENTS a response from occuring
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Schedule I: Controlled Drugs
- High abuse potential, no accepted medical use.
- Ex: Heroin, Marijuana, LSD, Mescaline (peyote), Cocaine
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Schedule II: Controlled Drugs
- Narcotics: Written Prescription. No telephone refills. High abuse potential. Accepted medical use.
- EX: Opium, morphine, codeine, methadone, meperidine, secobarbital, amphetamine)
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Schedule III: Controlled Drugs
- Moderate Abuse. Non narcotic derivatives. Prescriptions can be rewritten after 6 months or 5 refills. Less abuse potential. low physical but high psycho dependance. Accepted medical use.
- EX: Androgens and anabolic steroids
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Scheduled IV: Controlled Drugs
- Less abuse potential. mild dependence. limited physical or psych dependence. Limit to 5 refills. written or oral prescription.
- Ex: Valium, phenobarbital, chloral hydrate, benzodiazepine, meprobamate
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Schedule V: Controlled Drugs
Preps containing limited opioids. Cough Syrups, antidiarrheals. Limited potential for abuse. prescription may be required, depends on state laws.
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Parenteral
IM, SQ, Interdermal, IV
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Drugs susceptible to first pass
Dopamine, imipramine, isoproterenol, lidocaine, morphine, nitroglycerin, propranolol, reserpine, warfarin
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Digoxin half life
33-44 hours
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Warfarin Half life
0.5-3 days
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Levothyroxin Half life
6-7 days
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Valium Half life
20-50 hours
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Dilantin half life
22 hours
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Narrow Therapeutic Index Drugs
- Dilantin
- Theophylline
- Lithium
- Coumadin (warfarin)
- Digitoxin
- Digoxin
- Aminoglycocides
- Insulin
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Sympathetic Nervous System
Fight or flight
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Parasympathetic Nervous System
Rest and digest
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Cholinergic drugs
act on the parasympathetic nervous system
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Cholinergic Crisis
overstimulation at the neuromuscular junction due to an excess of Acetylcholine
S/S: Respiratory failure, flaccid paralysis, excessive salivation and perspiration
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Drugs that block the effect of ACH
- Anticholinergics
- parasympatholytics
- cholinergic antagonists
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Atropine Sulfate
Cholinergic Antagonist
Use: Emergency use, bradycardia, pulseless electrical activity, asystole, cpr, decrease resp. secrestions, induction of mydriasis
Contraind: hypersensitivity, myasthenia gravis, acute MI, glaucoma
SE: Blurred vision, dry mouth, constipation, urinary retention (CRUCIAL TO MONITOR)
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Anticholinergic OD
mad as a hatter (CNS PSYCHOSIS) dry as a bone (SALIVARY) red as a beet (VASODILATION) blind as a bat (MYDRIASIS)
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Alpha 1
eyes, blood vessels, bladder, male sex organs
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Alpha 2
Pre synaptic nerve terminals
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Beta 1
primarily the HEART, but also kidneys
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Beta 2
arterioles of the heart, LUNGS, and skeletal muscles, bronchi, uterus, liver
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Alpha 1, Beta 1 responds
to EPI, NE, Dopamine
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Alpha 2 responds
to EPI , NE
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Drugs that mimic norepinephrine
- Adrenergics
- SympathoMIMEtics
- Adrenergic Agonist
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Epinephrine
Use: wide variety, asthma, shock, etc
Admin: parentally, topically or by inhalation
- Metabolized: liver
- Pregnancy CAT C
Absorption: tissues
Excreted: Kidneys
Duration: 1-4 hours
Stimulates ALL adrenergic receptors
Contraind: hypersensitivity, sulfite sensitivity, close angled glaucoma, labor
AE: HTN Crisis, angina, cerebral hemorrhage, cardiac arrythmias
Drug Interaction: tricyclic antidepressants, oxytocics, halogenated anesthetics and beta blockers
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Block effects of NE
- Sympatholytics,
- adrenergic blockers,
- adrenergic antagonists
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Propranolol (Inderol)
Beta blocker
USE: HTN, Angina, MI, Migraine, essential tremor, situation anxiety, substance withdrawal
- b1: decreases heart rate
- b2: bronchospasm
given orally or IV
Contraind: bradycardia, heart block, airway disease, raynaud syndrome, antidepressant use
SE: Myocardial ischemia if stopped suddenly, infarction, htn, angina, depression, diarrhea
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Digoxin (Lanoxin)
Use: treatment of CHF, AFIB, Tachycardia
Admin: Oral, IV
Excreted: Kidneys
Contraind: heart block, vfib, hypersensitivity
AE: Dysrhythmias, anorexia, n/v/d, HA, wkns, apathy, drowsiness, visual disturbances, confusion, restlessness, disorient, seizures, delirium, hallucinations, neuralgia, psychosis
Drug Interactions: Multiple drugs
Check intake of K+, Ca, Mg.
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Fasting Blood Glucose Values
Under 100mg/dl
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Gentamicin Lab Value
5 to 10
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Creatine Lab Value
0.84 to 1.21
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Digoxin Lab Value
0.5 to 2.0
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Potassium Lab Value
3.6 to 5.2
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T3 Lab Value
- T3 free 0.2-0.5 ng/dl
- T3 total 75-195 ng/dl
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T4 Lab Value
5.0 to 12.0 mcg ug/dl
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Dilantin Lab Value
10 to 20 ug/ml
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TSH Lab Value
0.4 to 4.0 mu/L
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Drugs must be ________ to enter the BBB
ipophilic or have a transport system
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Glomerular Filtration
- Drugs enter capillaries surrounding Bowman’s capsule
- Most drugs move easily through capillary walls and into the proximal tubule (urine)
- Proteins cannot pass
- If drug molecules are still bound to protein, they will not pass and can lead to toxicity.
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Phosphodiesterase (PDE Inhibitors)
- Inamrinone (Inocor)
- Milrinone (Primacor)
short term management of heart failure, long term management of pt's awaiting heart transplant
given IV, only used when other meds are not working
reduce K+
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Catopril (Capoten)
ace inhib:
use: antiHTN
Contraind: hypersensitivity
SE: Dry non productive cough, HA, Fatigue, Increased k+
Edu: 1h ac, rise slowly, photosensitivity, do not take k+ supps
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Antianginals
reduce myocardial o2 demands by increasing o2 to heart or both
- ex: nitrates
- beta blockers
- ccb's
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Beta Blockers
- Propranolol (inderal)
- Atenolol (Tenormin)
- Metoprolol (Lopressor)
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Calcium Channel Blockers
- Verapamil (Calan)
- Diltiazem (Cardizem)
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Phase 1: Drug Development
drug tested on healthy volunteers to make sure the drug can be given safely to people. 20-80 volunteers.
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Phase 2: Drug Development
100-300 volunteers who have the disease for which the drug is thought to be effective.
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Phase 3: Drug Development
Large number of patients, 1000-3000 in medical research centers receive the drug. Provides info about infrequent or rare side effects. Double blind study.
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Phase 4: Drug Development
Voluntary. Post market surveillance of the drugs therapeutic effects.
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Cholinergic LESSDUMB
- lacrimination
- excitation of nicotinic receptors
- salivaiton
- sweating
- diarrhea
- urination
- micturition
- bronchoconstriction
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IDEA Cardiac Arrest
- Isoproterernol
- Dopamine
- Epiniphrine
- Atropine
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Left HF
- coughing
- hematotisis
- orthopnea
- pneumonia
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Right HF
- splenomegaly/hepatomegaly
- edema
- ascites
- distended neck veins
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Best drug for HTN crisis?
Nipride
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Best drug for edema?
Furosemide (lasix)
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The sympathetic nervous system produces what type of response?
Adrenergic
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Adrenergic class drugs/receptors
Beta 1, Beta 2, Alpha 1, Alpha 2
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Drugs that Mimic acetylcholine
- Cholinergic
- Parasympathomimetics
- Cholinergic agonists
- Cholinergic stimulants
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Muscarinic Agonist
Bethanechol (Urecholine)
•Use: postoperative urine retention and retention caused by neurogenic atony of bladder
•Contraindications: inflammatory lesions on GI tract, bronchial asthma, CAD, hypertension,
•Side effects: overstimulation of the PNS what does that look like?
•No not give IM or IV because of risk for cholinergic crisis
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Neurotransmitter for SNS
Norepinephrine
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Direct acting
directly stimulate adrenergic receptors
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Indirect acting
stimulate the release of norepinephrine from nerve endings into the synapse
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Dual acting
stimulates both adrenergic receptor and release of norepinephrine
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Phenylephrine (Dristan)
Alpha 1 Agonist
Use: vascular failure in shock, drug induced hypotension. SVT, Nasal congestion, mydriasis (dilation)
•Contraindication: drug hypersensitivity, severe hypertension, VT, glaucoma
•Side Effects: HA, restlessness, excitability, reflex bradycardia
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Clonidine (Catapres)
Alpha 2 Agonist
•Use: management of hypertension
•Contraindication: hypersensitivity
•Side effects: agitation, dizziness, drowsiness, fatigue, HA, CP, hypotension, decreased libido
•Education: Rise slowly, position changes
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Isoproterenol (Isuprel)
Beta Agonist
Use: Beta 1 Bradycardia (positive inotropic and chronotropic effects) Beta 2 treat bronchospasm in asthma and prevent bronchospasm in COPD
•Contraindication: angina, hypersensitivity
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Prazosin (Minipress)
Alpha Blocker
•Use: management of refractory chronic heart failure, Raynaud vasospasm, prostatic outflow obstruction, hypertension
•Contraindication: hypersensitivy, angina pectoris (severe hypotension)
•Side Effects: light headedness, dizziness, HA, weakness
•Given orally
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CHF Class 1
patients are asymptomatic and have no limitation of thier activities
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CHF Class II
patients are short of breath or fatigure with moderate activity such as climbing two flights of stairs, slight limitation
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CHF Class III
patients are short of breath or fatigued with very mild exertion activity such as climbing one half flight of stairs and are only comfortable at rest, limited activity
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CHF Class IV
patients are exhausted short of breath or fatigued at rest
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Cardiac Glycosides
Can be given PO or IV, absorption rate 70%, low protein binding, excretion 70% in urine 30% by liver, Peak 6-8 hours, PO onset 30min to 5 hours, IV 10 to 30 min, Peak 1 to 5 hours
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ACE inhibitors
- catopril
- lisinopril
- DO NOT GIVE PRILS TO PREGNANT WOMEN
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Lisinopril
Treats Heart failure and HTN.
May take 2-3 mo for heart to get to optimal functioning---
Increased survival for pts if they get a dose within 24 hrs after an acute MI
Combine hydrochlorazide ( diuretic) with Lisinopril.
Unlabelled use - migraines
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Beta adrenergic antagonists
- all beta blockers ending with olol
- propanolol
- atenolol
- metropolol
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Calcium Channel Blockers for?
Used to prevent angina that does not respond to other drugs. Can also be used as antiarrhythmics and antihypertensives
For long term use only
Prevent the passage of calcium ions across the myocardial cell membrane and vascular smooth muscle cells
Causes dilation of the coronary and peripheral arteries
Decreases the force of the hearts contraction and reduces workload
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CCB Drugs
- Verapamil (Calan)
- Dilitiazem (Cardizem)
- Amlodipine (Norvasc)
- Bepridil (Vascor)
- Nifedipine (Procardia)
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Angiotension II Receptor antagonists (blockers) ARB Losartan
Adverse Reactions: headache, fatigue, cough, angioedema, increased serum potassium
Check BP, Pulse prior to giving
Monitor fluid/electrolyte status
Monitor for hypotension, or positional blood pressure changes (safety)
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Direct Vasodilators Apresoline-Hydralazine
Use: antihypertensive
Acts similar to nitrates EXCEPT hydralazine is selective for arteries
Contraindications: angina, MI, tachycardia. Lupus.
Take with food
Monitor BP and pulse regularly, Tolerance can develop.
Discontinue immediately if Pt has lupus-like symptoms (arthralgia (joint pain), fever, myalgia, pharyngitis, splenomegaly)
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ACE Inibitos only do what?
lower BP, can be given if pulse is below 60
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Beta Blockers Neg?
- Chronotropic-lower rate
- inotropic-less force
- dromotropic-less beats
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Beta blockers decrease?
- worklord
- resistance
- cardiac output
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CCB avoided in?
patients with CHF
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