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Drug
any chemical that affects living processes
Pharmacology
the study of drugs and their effects on living processes (plants, body tissues, etc.)
Clinical Pharmacology
the study of drugs in HUMANS
Pharmacotherapeutics
the use of drugs to diagnose, prevent, and treat illnesses as well as to prevent pregnancy
Minimal Effective Concentration
the smallest dose of a drug that produces the desired effect
Toxic Concentration
the dose of a drug that produces toxic effects
Therapeutic Range
between the MEC & the TC; gets desired effect(s) from drug without toxic side effects
P450 System
an enzyme that alters drug metabolism
-accelerates renal excretion
-inactivates drug
-enhances drug
-activates prodrugs
Prodrugs
drugs that are not activated (inert) until they pass through the liver
First-pass Effect
deactivation of drug by liver after GI absorption
Drug Half-Life
time it takes for drug levels to decrease by 50%
-it takes five half-lives to maintain a normal therapeutic range
Loading Dose
drugs with short half-lives get a larger initial dose in order to achieve therapeutic range
Maintenance Dose
small doses given to maintain therapeutic range
ED50 (Average Effective Dose)
the dose that produces the desired effects in 50% of the population
Therapeutic Index
= LD50 / ED50
-average lethal dose / average effective dose
-the higher the number, the safer the drug
Alpha1 Receptors
Sympathetic
-Adrenergic Receptor
-vasculature
-vasoconstriction
-pupil dilation
-ejaculation
-bladder neck contraction
Alpha2 Receptors
Sympathetic
-Adrenergic Receptor
-minimal
Beta1 Receptors
Sympathetic
-Adrenergic receptor
-heart & kidney
-increase HR, force of contraction & velocity of conduction
-Renin release
Beta2 Receptors
Sympathetic
-Adrenergic receptor
-bronchodilation
-relaxation of uterine muscle
-glycogenolysis
Nicotinic n
Paraympathetic
-cholinergic receptor
-promotes release of epinephrine
Nicotinic m
Parasympathetic
-cholinergic receptor
-contraction of skeletal muscle
M1 Receptor
Parasympathetic
-cholinergic receptor
-muscarinic
-salivary/CNS
-increases salivation and cognition
M2 Receptor
Parasympathetic
-cholinergic receptor
-muscarinic
-heart
-bradycardia
M3 Receptor
Parasympathetic
-cholinergic receptor
-muscarinic
-salivary, GI, bladder, eye
-increases salivation
-increases gastric secretions, tone & motility
-contracts detrussor muscle
-pupil constriction
drug of choice for bradycardia?
ATROPINE
-given for muscarinic poisoning (mushrooms)
-anti-cholinergic
-muscarinic antagonist
-increases HR
-increases secretions (good for pre-anesthesia)
-dilates pupils (eye surgery)
Myesthenia Gravis
auto-immune process against nicotinic m receptors on skeletal muscle
-muscle weakness (including respiratory muscles)
Neostigmine/Prostigmin
myesthenia gravis
-inhibits ACh
-works peripherally
Parkinson's disease
neurodegenerative disorder
-loss of dopaminergic neurons in basal ganglion
-decreased dopamine
-rigidity, mask-like face, tremor, instability, bradykinesia
Levodopa/Dopar
Parkinson's disease
-precursor to dopamine
-metabolized into dopamine in the brain
-only 2% makes it into brain
-initially effective but diminishes over time due to advancement of disease & tolerance
-side effects: N/V, hypotension, dysrhythmias
-do not give to patients taking MAO-inhibitors (can cause hypertensive crisis)
Sinemet
Parkinson's disease
LEVODOPA + CARBIDOPA
-Carbidopa blocks metabolizing of Levodopa in gut
-allows more to gross BBB into the CNS
-able to decrease Levodopa dose
Dopamine Agonists
Parkinson's disease
-increases activation of dopamine receptors
-less effective than dopamine itself
Dopamine Agonists: Ergot Derivatives
Parkinson's disease
-less selective for dopamine receptors
-more side effects
Dopamine Agonists: Non-Ergot Derivatives
Parkinson's disease
-more selective for dopamine receptors
-less side effects
Alzheimer's Disease
Neurodegenerative disorder
-progressive memory loss
-neuromotor decline
-starts in Hippocampus (limbic system) and progresses to cerebral cortex
Cholinesterase Inhibitors
Alzheimer's disease
-for mild symptoms
-prevent breakdown of ACh
-patients don't respond well
-cholinergic side effects (dec. HR & BP, diarrhea, salivation)
NMDA Receptor Antagonists
Alzheimer's disease
-for severe symptoms
-better tolerated than CI
-decrease in symptoms, may slow progress
-blocks flow of calcium into memory cells
Procaine/Novocain
Lidocaine/Xylocaine
Local anesthetics
-Novocain -> metabolized in blood
-Xylocaine -> metabolized in liver
-pain lost first, then temp, touch, & deep pressure
-DO NOT USE CENTRALLY!!! May effect cardiac function
-give with epinephrine to contain drug at site (vasoconstriction)
Propofol/Diprivan
Anesthetic
-lipid-based
-conscious sedation
-hypotension & risk for infection (because of lipid-based nature)
-given IV
Narcotics
opioid analgesics
-analgesia, resp. depression, sedation, euphoria, constipation, vasodilation
-be careful with possible dependence
-Morphine, Dilaudid, Oxycodone/Percocet
antidote for narcotic overdose?
NALOXONE
two types of drugs for Asthma?
anti-inflammatory & bronchodilation
Glucocorticoids for Asthma
anti-inflammatory action
-given via inhalation to decrease systemic effects
-IV push for emergency
-PO can cause adrenal insufficiency (wean off)
prophylaxis for chronic asthma
Leukotriene Modifiers for Asthma
anti-inflammatory action
-suppress actions of leukotriene (bronchoconstriction, edema)
-can cause liver toxicity
Cromolyn/Intal for Asthma
anti-inflammatory action
-suppresses bronchial inflammation
-inhibits inflammatory cells
-decreases release of histamine
-not for acute episodes, for prophylaxis BEFORE EXERCISE
Beta2 Agonists for Asthma
bronchodilation
-combine with inhaled glucocorticoids
-relaxes smooth muscle
Albuterol/Pronventil
SABA (for Asthma)
-use for acute attacks
-immediate
-lasts 3-5 hrs
Salmeterol/Serevent
LABA (for Asthma)
-given DPI (dry-powder inhaler)
-mortality r/t excessive use
-lasts 12 hrs
-prophylactic
Natriuretic Peptides
for hypertension
-responds to fluid overload
-vasodilation
-reduces blood volume
-may get overwhelmed by HF progression
ACE Inhibitors
Hypertension, HF, MI/stroke prevention
"-PRILS"
-pro-drug
-reduce dose in renal disease/toxicity
-vasodilation. stops production of angiotension II (& therefore aldosterone) which decreases blood volume
-first-dose hypertension, fetal injury (not given to pregnant women)
giving ACE Inhibitors will cause renal failure in patients with __________________.
renal artery stenosis
If we inhibit ACE, we inhibit _______, therefore promoting ______________
-inhibit Kinase II
-promotes Bradykinin
-will cause angioedema and a barky cough
Calcium Channel Blockers
hypertension
-decreases BP via vasodilation
-2 kinds
Procardia
Calcium Channel Blocker
-affects arterioles
-angina, hypertension, migraine prophylaxis
-acts on arteriole smooth muscle (vasodilation)
-reflex tachycardia
Cardizem
Calcium Channel Blocker
-affects arterioles & heart
-vasodilation
-decreases rate, force of contraction & velocity of conduction
-no reflex tachycardia (because of affect on heart)
drug of choice for atrial fibrillation?
DELTIAZEM/CARDIZEM
Beta Blockers
used for hypertension, HF, dysrhythmias
-NEVER GIVE BETA BLOCKERS TO A PATIENT WITH AN AV HEART BLOCK!!!!!!!!!!!!!!!
Selective Beta Blockers
works only on beta1 receptors (only on heart)
-Metoprolol
Nonselective Beta Blockers
works on both beta1 & 2 receptors
-cheap
-but have to worry about effects on lungs
Nitroglycerin
ANGINA
-acts directly on vascular smooth muscle
-dilation of arterioles
-side effects: hypotension, headache
-sublingual is best
-oral for prophylaxis
-IV for short-term use only
-transdermal -> remove patch at night (period of least activity)
Heparin
Anti-Coagulant
-given IV
-monitor PTT (prolonged thromboplastin time)
-risk for bleeding
-HIT (Heparin-induced thrombocytopenia)
antidote for heparin?
protamine sulfate
Low Molecular Weight Heparins
-administered SC
-do not have to monitor levels
-can be done at home
Warfarin/Coumadin
Anti-Coagulant
-given PO
-vitamin k antagonist
-monitor PT (prothrombin time)
antidote for Warfarin/Coumadin?
vitamin K
Plavix
Anti-Platelet
-prevents platelet aggregation
-risk for bleeding
Glycoprotein IIb/IIIa Receptor Antagonist
-reversible blocking to prevent aggregation
-IV short-term in combo with ASA & Heparin
-Abciximab/ReoPro
Pletal
-platelet inhibitor for INTERMITTENT CLAUDICATION
Persantin
-used for prevention of thromboembolism FOLLOWING A HEART VALVE REPLACEMENT
Lasix
Loop Diuretic
-VERY high urine output; hypokalemia
Thiazide Diuretics
-high urine output
-need good renal function
-do not give to patients with gout
Potassium-Sparing Diuretics
Aldactone
-often used in combo with Lasix to save K+
-small urine output
-preserves K+
Osmotic Diuretics
Mannitol
-moves intracellular fluid into vascular space
-must be given IV
-inhibits reabsorption of H2O
-cerebral edema
Statins (HMG-CoA Reductase Inhibitors)
-reduce LDL & increases HDL
-take in evening (most cholesterol production is done at night)
-every-other-day dosing is used to manage side effects
-side effects: MYOPATHY & muscle pain
drug of choice for hypertensive emergencies?
NIPRIDE
drug of choice for SVT (supraventricular tachycardia)?
ADENOSINE
-quickly in repeated IV Push doses
-follow with normal saline
drug of choice for anaphylaxis?
EPINEPHRINE
Type I Diabetes
Insulin-Dependent Diabetes
-no insulin produced
Type II Diabetes
non-Insulin Dependent Diabetes
-strongly related to obesity
-insulin resistance or impaired insulin secretion
Humalog / Novolog
Short Duration: Rapid-Acting
-bolus
-clear preparations
-given with meals
-SC & via pump
Humulin / Novolin
Short Duration: Slower Acting
-clear prepartions
-SC, IM, IV, and via pump
-given with meals
Novolin N / Humulin N
Intermediate Acting
-NPH (cloudy preparations)
-SC only
Levemir / Lantus
Long-Duration
-DO NOT MIX
-lasts 24 hours
-clear
-SC only
Sulfonylureas
PO DM Drug
-Type I
-promote insulin by pancreas
-caution in patients with sulfa allergy!
Meglitinides (Glinides)
PO DM Drug
-promote insulin secretion by the pancreas
-take with meals 2-3 times a day
-DO NOT USE WITH LOPID (A STATIN)!!!!!!!!!!!!!!!!!!!!!!!
oral drug of choice for diabetes??
Biguanides
Biguanides
PO DM Drug
-METFORMIN
-Type II Diabetes
-decrease glucose production by liver
-increase glucose uptake by muscle
-GI side effects (diarrhea)
-off-label use for polycystic ovarian syndrome
Thiazolidinediones (Glitazones/TZDs)
PO DM Drug
-add-on for biguanides
-decreases insulin resistance (type II)
-need insulin present to work
-weight gain r/t fluid retention
Alpha-Glucosidase Inhibitors
PO DM Drug
-inhibits carbohydrate digestion/absorption
-decreases postprandial hyperglycemia
-side effects: flatulence, cramps, diarrhea
DPP4 Inhibitors (Gliptins)
PO DM Drug
-enhances action of incretin
-inhibits glucagon
-adverse effects: pancreatic cancer, pancreatitis
GLP-1 Receptor Agonists
PO DM Drug
-Incretin mimetic
-only available SC
-hypoglycemia/pancreatitis
Symlin
PO DM Drug
-type I & II
synthetic amylin
-side effects: nausea, weight loss, severe hypoglycemia
Sodium Glucose Cotransporter 2 (SGLT2) Inhibitors
PO DM Drug
-"peeing out glucose"
-newest class of PO medications
Histamine 2 Receptor Blockers
Peptic Ulcers
-Tagamet
-suppress secretion of gastric acid
-H2 receptors in the parietal cells of stomach
-CNS side effects (confusion, CNS depression/excitation)
-pneumonia is common side effect
Proton Pump Inhibitors (PPIs)
Peptic Ulcers
"-prazole"
-most effective in suppressing gastric acid secretion
-blocks generation of acid
-IRREVERSIBLE (lasts longer!)
-side effects: rebound hypersecretion, c diff, hypermagnesemia
Sucralfate/Carafate
Peptic Ulcers
-inert
-provides protective barrier between acid & epithelium
-may effect absorption of other drugs (dilantin, warfarin, etc.)
Antacids
-alkaline compounds
-neutralize gastric acids (bring pH up)
which antacids can cause diarrhea?
MAGNESIUM compounds
which antacids can cause constipation?
ALUMINUM compounds
Group I Laxatives
water stool in 2-6 hours
Group II Laxatives
semi-fluid stool in 6-12 hours