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    Pharm Exam#1

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    skollkoll
    This document provides a review of key topics in pharmacology, including: - Drug uses such as diagnostics, prevention, treatment and cure - Factors affecting drug absorption, distribution, metabolism and excretion - Classes of drugs like adrenergic agents, cholinergic agents, bronchodilators and antihypertensives - Mechanisms of action and side effects of many common medications

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    Pharm Exam#1

    Uploaded by

    skollkoll
    183 views13 pages
    This document provides a review of key topics in pharmacology, including: - Drug uses such as diagnostics, prevention, treatment and cure - Factors affecting drug absorption, distribution, metabolism and excretion - Classes of drugs like adrenergic agents, cholinergic agents, bronchodilators and antihypertensives - Mechanisms of action and side effects of many common medications

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    This document provides a review of key topics in pharmacology, including: - Drug uses such as diagnostics, prevention, treatment and cure - Factors affecting drug absorption, distribution, metabolism and excretion - Classes of drugs like adrenergic agents, cholinergic agents, bronchodilators and antihypertensives - Mechanisms of action and side effects of many common medications

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    183 views13 pages

    Pharm Exam#1

    Uploaded by

    skollkoll
    This document provides a review of key topics in pharmacology, including: - Drug uses such as diagnostics, prevention, treatment and cure - Factors affecting drug absorption, distribution, metabolism and excretion - Classes of drugs like adrenergic agents, cholinergic agents, bronchodilators and antihypertensives - Mechanisms of action and side effects of many common medications

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    © All Rights Reserved
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    Thursday, December 5, 2013

    Pharmacology Exam 1 Review


    Introduction to Pharmacology

    - Drug Usages
    Diagnostics
    - Glipizide: lowers blood sugar > diagnostics for DM
    - Phentolamine and Phenoxybenzamine: diagnosis and treatment of
    pheochromocytoma

    Prevention, treatment, and cure


    Placebo Effects
    - Production of an effect independent of the chemical nature of the substance
    Lactose capsules
    - Pure placebo: lactose capsules or NaCl injection
    - impure placebo: drug has another effect but not intended
    ASA, B12, and Vitamin C
    - Absorption
    Weak acid: absorbed in the stomach
    - anything with Sodium
    Weak base: absorbed in the intestines
    - anything with HCL or sulfate
    Thiopental
    - highly lipid soluble > CNS entrance
    - rapidly redistribute through muscle and brain
    Rapid onset of action and shortest duration of action
    - Used as pre-anesthetic
    Factors
    - Depends on the physicochemical properties of molecule
    pKa and pH
    - Site of administration
    1

    Thursday, December 5, 2013

    Injection gives 100%


    - Formulation of drug
    Liquid, elixirs, and syrups: Fastest
    Tablets: slowest
    - Food or fluids administered with the drug
    Tetracycline with dairy products = inhibit absorption
    Anti-fungal = enhance absorption
    - Route
    Enteral
    - via mucosa and GI
    - Oral, sublingual, buccal, and rectal
    - Subjected to the First-Pass effect
    drugs are subjected to the liver metabolism
    IV can bypass the liver, thus preventing the metabolism
    - IV, rectal, sublingual, Subcutaneous, transdermal, IM
    - Rectal
    Poor absorption surface
    Parenteral
    - IV, IM, SC,
    IV is the fastest delivery into the blood circulation
    Topical
    - Skin, eyes, ears noses, and lungs
    - Lidocaine and epinepherine
    - Depo form = use solubility to delay absorption
    - Benzethine + Penicillin G > Longer acting
    - Distribution
    Transport of a drug in the body by the blood stream to its site of action
    protein-binding
    - decreases bioavailability, but increases the duration of action
    2

    Thursday, December 5, 2013

    Areas of rapid distribution: heart, liver, kidneys, and brain


    Areas of slow distribution: muscle, skin, fat
    Factors affecting distribution
    - Lipophilicity:
    - Drug molecule size
    - protein binding
    drug-drug interaction
    - warfarin with Aspirin > rapid increase in warfarin = increase in bleeding
    - rate of metabolism
    - other binding sites
    Blood Brain Barrier
    - thiopental crosses BBB
    - high lipid solubility = unable to cross BBB
    - Metabolism
    biological transformation of a drug into an inactive metabolite, a more soluble
    compound, or a more potent metabolite

    liver, kidney, lung, plasma, intestinal mucosa


    factors deceasing metabolism:
    - renal insufficiency
    - CV dysfunction
    - Slow acetylator
    - Erythromycin and ketoconazole - Enzyme inhibitors
    - Cimetidine
    Factors that increase metabolism: Enzyme inducers
    - Barbiturates - Phenobarbital
    - Fast acetylators
    - Rifampin
    - carbamazepine
    Effects
    3

    Thursday, December 5, 2013

    - delayed drug metabolism: accumulation of drugs


    prolonged action of the effects of the drugs
    - Stimulation of drug metabolism
    diminished pharmagologic effects
    - Phase 1 reactions
    Hydroxylation, oxidation, deamination, etc
    - Phase 2 reactions
    conjugation
    Pro Drug
    - the drug requires the activation by the liver
    - Chloral Hydrate - Pro-drug
    -> Triclorethanol = activated drug
    Need Functional liver
    - Excretion
    ionized drugs: excreted in urine
    Hyperuricemia:
    - Probenecid binds to uric acid for excretion
    Used with penicillin for effectiveness
    Toxicity
    - ASA or weak acid overdose = Sodium Bicarbonate
    - Weak base Overdose = Vitamin C or ammonium chloride
    Enterohepatic Cycling
    Pseudocholinestersases - Deficiency > Paralysis
    - Tolerance
    decreasing response to repetitive drug doses
    mechanism: enzyme induction
    Bretylium: for tachyphalaxsis > rapid tolerance in 10mins
    Adrenergic Agonists and Antagonist
    4

    Thursday, December 5, 2013

    - NE = main NT
    - multiple short pre-ganglionic to long post ganglionic nerves
    - Adrenergic Agents: MOA
    Direct Acting: binds directly to the receptor and causes physiologic response
    Indirect acting: causes the release of catecholamine
    Tyramine like effect
    - MAOI with tyramine foods > hypertensive crisis
    - Tyramine: by product of tyrosine metabolism
    - Synthesis of NE
    Tyrosine > L-DOPA > Dopamin > NE
    Tyrosine Hydroxylase > Dopa Decraboxylase > Dopamine Beta-Hydroxylase
    Cocaine = inhibits reuptake of NE = Sympathomimetic
    Ampthetamine = increase NE release = Sympathomimetic
    - Destruction of NE
    Reuptake of NE
    COMT - membrane bound enzyme
    MAO -> pre-synaptic are of post ganglionic
    Major Metabolite = VMA - excreted in urine
    Guanethidine: inhibits secretion of NE = Sympatholytic
    Reserpine = depletes NE at the storage granule = Sympatholytic
    - Alpha 1 Receptors
    Located on postsynaptic effector cells
    Effects:
    - Vasoconstriction and CNS stimulation
    - GU: Constriction of Sphincter and Uterus Contraction
    - Decreased insulin release
    - Pupillary contraction via ciliary muscle contraction
    Side Effects:
    - CNS: Euphoria, excitement, insomnia
    5

    Thursday, December 5, 2013

    - CV: palpitations, tachycardia, vasoconstriction


    - Beta 1 Receptors
    located in the heart
    - Stimulation of heart
    Effects:
    - Heart
    AV node = Increased heart rate
    SA node = Increased heart rate
    Increased force of contraction - Inotropic
    Increased heart rate - chronotropic
    Increased conduction through AV node - dromotropic
    - Anorexiants:
    Benzphetamine
    Dextroamphetamine
    Dexerdrine
    - GI: Sphincter constriction
    - Beta 2 receptors
    located in smooth muscle of the bronchioles, arterioles, and visceral organs
    - Relax smooth muscle = bronchodilation + Vasodilation + uterine relaxation
    Effects:
    - GI = decreased motility
    - Bronchial Dilation
    - Uterine relaxation
    - Glycogenolysis = increase in beta
    - Catecholamine Substitutions
    - Methylation at the Amino group = increase in beta activity
    NE : 95:5 > Epi: 50:50
    - Alpha Blockers
    Uses:
    6

    Thursday, December 5, 2013

    - Vasodilation - reduction in BP
    - decreased bladder contraction - BPH
    - Pheochromocytoma
    - Raynauds
    Side Effects:
    - CV: Palpitations, orthostatic Hypotension, tachycardia
    - CNS: drowsiness, dizziness
    - GI: constipation
    - Incontinence
    - Beta Blockers
    Beta 1
    - Decreased heart rate,
    - slows conduction rate
    - decreases myocardial oxygen demand
    Beta 2
    - Vasoconstriction, Bronchiole constriction
    Uses:
    - Anti-agina, cardioprotective, Glaucoma, hypertension,
    Side Effects:
    - bronchocontriction, bradycardia, hypoglycemia, rebound hypertension
    Cholinergic Agonists and Antagonists

    - Muscarinic Receptors
    locations: Smooth muscles, cardiac muscle, glands
    Simulation intestine and bladder
    - Increased motility, secretion, and urinary frequency
    Stimulate pupil
    - Constriction and reduced intraocular pressure
    Increased salivation and sweating
    7

    Thursday, December 5, 2013

    Vasodilation and decreased heart rate


    Bronchial Constriction
    - At recommended doses: affects the muscarinic receptors
    Higher doses: nicotinic Receptors
    Muscarinic: desired effects
    - Uses
    Glaucoma
    Bladder and GI motility increase
    Alzheimers
    - Side Effects:
    Bradycardia, hypotension
    headache
    bronchospasms and increased bronchial secretions
    - Cholinergic Antagonists
    CV: Increase heart rate
    CNS: drowsiness
    EYE: pupil dilation + cycloplegia
    GI: decreased muscle tone, peristalsis, and secretions
    GU: increased constriction = retention
    Bronchialdilation
    - Side Effects
    CV: increased HR
    CNS: CNS excitation
    Dilated pupils with cycloplegia
    Urinary Retention
    decreased bronchial secretion
    Higher risk for heat stroke due to lack of sweating
    - EYE
    Glaucoma
    8

    Thursday, December 5, 2013

    - Ciliary muscle contraction


    cholinergic
    - Decreased secretion
    Beta-blockers
    - Decreased secretion due to HCO inhibitor
    diuretics
    Eye dilation
    - Atropine or cholinergic blockers = cause cycloplegia
    - adrenergic drugs = NO cycloplegia
    Bronchodilators

    - Xanthine Derivatives
    Theophylline
    - Increases the levels of cAMP by inhibiting PDE > bronchodilation
    - also causes CNS stimulation and cardiovascular stimulation
    MILD TO Moderate asthma + COPD
    SE:
    - Nausea vomiting, GERD, tachycardia,
    - Beta - agonists
    sympathomimetics
    Acute phase of asthmatic attacks
    - quick dilation of bronchiole
    Types
    - Non-selective
    Simulate both alpha and beta
    Epinepherine
    - Non-selective beta-adrenergics
    both beta 1 and 2
    Isoproterenol
    9

    Thursday, December 5, 2013

    - Selective beta 2
    albuterol
    - loses specificity at larger doses
    - Side Effects:
    NS and B1+2
    - cardiac stimulation
    Albuterol
    - tremor
    - Anti-cholinergics
    Prevention of brochoconstriction
    slow and prolonged action: used for prevention of bronchospasm
    SE: dry mouth, GI distress, and coughing
    - Antileukotrienes
    prevention of leukotrienes from attaching to receptors on cells
    - prevention of inflammation
    For: prophylaxis and chronic treatment of asthma
    NOT for acute
    SE: liver dysfunction
    - Corticosteroids
    Anti-inflammatory
    Only for Chronic asthma
    - do not relieve symptoms of acute asthmatic attacks
    - Not considered as first-line agents
    SE: pharyngeal irritation and fungal infections
    - Mast cell stabilizers
    Indirect-acting agents that prevents release of the various substances
    ONLY for prophylaxis, Not for acute
    Anti-hypertensive agents
    10

    Thursday, December 5, 2013

    - Hypertension Classification
    Normal: 130/85
    High Normal: 130~139/85~89
    Stage 1: 140-159/90~99
    Stage 2:160-179/100~109
    Stage 3: 180-209/110~119
    Stage 4: 210/120
    - Diuretics
    Thiazide diuretics: HCTZ > early distal tubules
    Potassium sparing diuretics > late distal tubules
    - SE: hypokalemia
    mild to moderate hypertension
    Relative Indications:
    - heart failure and systolic HTN
    - Adrenergic Agents
    Alpha 1 blockers
    - SNS is not stimulated
    - Uses:
    BPH
    severe CHF with diuretics
    Centrally acting adrenergic
    - alpha 2 agonists
    - MODERATE TO SEVERE hypertension
    - Uses:
    hypertension
    menopausal flushing, glaucoma
    - Other indications:
    heart failure, migraine, tachycardia, angina
    Peripheral Acting Blockers
    11

    Thursday, December 5, 2013

    - Inhibit release of NE or depletion of NE stores


    - treatment of hypertension
    - ACE inhibitors
    used as FIRST LINE agents
    -pril
    Uses:
    - Hypertension
    - CHF
    - slows the progression of left ventricular hypertrophy after an MI
    Captopril +Trandolapril
    - Renal protective effects in patients with diabetes
    Ramipril + Captopril + Enalapril
    SE:
    - fatigue, dizziness
    - coughing, due to bradykinin
    Other indications
    - DM, nephropathy, HF, previous MI
    - A II Receptor Blockers
    No coughing
    -sartan
    Uses:
    - Hypertension
    SE:
    - headache, upper respiratory infection
    - Calcium Channel Blockers
    cause smooth muscle relaxation by blocking the binding of calcium to its receptors
    USES:
    - Angina, hypertension, Dysrhythmia, Migraine
    SE:
    12

    Thursday, December 5, 2013

    - Hypotension, palpitations, tachycardia


    - Constipation
    - rash and peripheral edema
    other indications
    - elderly systolic hypertension
    - Vasodilators
    may cause reflex tachycardia
    beta blocker should be used prior
    - Relative Indications
    Elderly: dihydropyridine or diuretic, no beta blockers
    African American: diuretics or Calcium channel blockers
    1st line stage 1: ARB with HCTZ

    13

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