Pharmacology Overview Part II

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Pharmacology Overview Part II

• Becca Maddox
• NURS 2205
• March 27, 2002

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Central Nervous System

• Consists of the brain and spinal cord
• Interprets the information sent by impulses from
  the PNS and sends back instructions to regulate
  body functions
• Drugs can either stimulate or depress the CNS

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CNS Stimulants

• Medically approved to treat
• Narcolepsy
• Attention deficit disorder in children
• Obesity
• Reversal of respiratory distress
• Major groups include
• Amphetamines and caffeine stimulate the
  cerebral cortex of the brain
• Analeptics and caffeine act on the brain stem
  and medulla to stimulate respiration
• Anorexiants act to some degree on the cerebral
  cortex and on the hypothalamus to suppress
  appetite
• Long-term use can produce dependence and
  tolerance
• Abruptly stopping CNS stimulants may result in
  depression and withdrawal symptoms

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AMPHETAMINES

• MOOD ELEVATION, INCREASE MENTAL ALERTNESS,
  DECREASED FATIGUE DROWINESS
• USED TO TREAT NARCOLEPSY ADD
• HIGH RECREATIONAL ABUSE

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ANALEPTICS/XANTINES

• Analeptics
• STIMULATE RESPIRATION WHEN THE NATURAL REFLEX IS
  LOST
• CAFFEINE (NO-DOZ)
• DOPRAM
• Xanthines
• RELAXS SMOOTH MUSCLE IN THE RESPIRATORY TRACT,
  DILATES PULMONARY ARTERIOLES STIMULATES CNS
• THEOPHYLLINE

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ANOREXIANTS

• SUPPRESSES APPETITES
• DIDREX
• PHENYLPROPANOLAMINE (DEXATRIM, ACUTRIM)

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TREATMENT OF ADD

• DEXTROAMPHETAMINE / AMPHETAMINES
• RITALIN
• Has the opposite effect, not understood

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SIDE EFFECTS

• CV - INCREASED HR, PALPITATIONS, HTN, ANGINA,
  ARRHYTHMIAS
• CNS - NERVOUSNESS, INSOMNIA, JITTERY
• GI - N/V/D
• GU - INCREASE FREQUENCY
• ENDOCRINE- INCREASED BMR

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ANOREXIANT / AMPHETAMINE

• TALK ABOUT AS A CNS STIMULANT
• BUT IS AN INDIRECT ALPHA AGONIST

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CNS DEPRESSANTS
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GENERAL ANESTHESIA

• OVERTON-MEYER THEORY
• THE GREATER THE LIPID SOLUBILITY THE GREATER THE
  EFFECT
• INITIALLY THE PATIENT LOSES THE 5 SENSES
  BECOMES UNCONSCIOUS
• MEDULLARY CENTER DEPRESSED LAST
• 4 STAGES OF ANESTHESIA

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MEDICATIONS (INHALANTS)

• ISOFLURANE
• HALOTHANE
• ENFLURANE
• NITROUS OXIDE - LAUGHING GAS

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GENERAL ANESTHESIA (PARENTERAL)

• Mixed class of drugs
• KETAMINE -produces a dissociative anesthesia
• used to do short procedures
• do not feel pain, auditory or visual stimuli
• ETOMIDATE

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LOCAL ANESTHESIA

• COMES IN MANY FORMS
• CAINES
• LIDOCAINE, CARBOCAINE, NOVACAIN, PONTOCAINE
• SQ INJECTIONS WITH WITHOUT EPINEPHRINE
• MIXED WITH IM ANTIBIOTICS

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HOW DO PAIN MEDICATIONS WORK?

• GATE THEORY
• SUBSTANCES ARE RELEASED (BRADYKININ, HISTAMINE,
  POTASSIUM, PROSTAGLADINS, SEROTONIN) WHEN TISSUE
  IS INJURED
• THEY TRAVEL ALONG THE NERVE FIBER ACTIVATE A
  PAIN RECEPTOR
• THIS TRAVELS UP THE SPINAL CORD A GATE ALLOWS
  THE IMPULSE TO GET TO THE BRAIN

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NARCOTIC ANALGESIC

• CLASSIFIED BY THEIR MECHANISM OF ACTION OR BY
  CHEMICAL MAKEUP
• CHEMICAL STRUCTURE - OPIATES
• MECHANISM OF ACTION - AGONIST, AGONIST-ANTAGONIST,
  PARTIAL AGONIST

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MECHANISM OF ACTION

• AGONIST - STIMULATES A RESPONSE
• AGONIST-ANTAGONIST - STIMULATES AT ONE RECEPTOR
  SITE BLOCKS AT ANOTHER
• PARTIAL AGONIST - STIMULATES A RESPONSE BUT NOT
  AS PRONOUNCED
• ANTAGONIST - NARCAN

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SIDE EFFECTS

• NARCOTICS WORK ON THE CNS BUT SIDE EFFECTS ARE
  OUTSIDE THE CNS
• DECREASED MOTILITY
• URINARY RETENTION
• RESPIRATORY DEPRESSION
• SUPPRESS THE MEDULLARY COUGH CENTER
• STIMULATES THE EUPHORIC HALLUCINATION RECEPTORS

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SIDE EFFECTS

• NAUSEA VOMITING
• PATIENTS OFTEN CONFUSE THE HISTAMINE RESPONSE AS
  AN ALLERGIC REACTION
• OPIOID TOLERANCE
• PHYSICAL DEPENDENCE

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THERAPEUTIC USES

• RELIEVE MODERATE TO SEVERE PAIN
• CONTROL DIARRHEA
• SUPPRESS COUGHING
• MAINTAIN BALANCED ANESTHESIA

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OPIATES

• PLANT SYNTHETIC
• THE CHEMICAL STRUCTURE CAUSES HISTAMINE TO BE
  RELEASED
• HISTAMINE CAUSES THE UNWANTED SIDE EFFECTS
• RASH, ITCHING, HYPOTENSION, DECREASED HEART RATE
• PLANT RELEASES MORE HISTAMINE - MSO4

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MEDICATIONS

• MORPHINE, MS CONTIN
• CODEINE
• DEMEROL
• METHADONE
• DILAUDID
• FENTANYL, DURAGESIC
• OXYCODONE
• PROPOXYPHENE

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AGONIST-ANTAGONIST

• TALWIN
• NUBAIN
• STADOL

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COMBINATIONS

• DARVOCET/WYGESIC, DARVON
• TYLENOL 3
• FIORINAL, FLORICET
• LORCET/VICODIN, LORTAB
• PERCOCET/TYLOX, PERCODAN
• ROXICET

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SEDATIVE-HYPNOTICS AGENTS

• HAS A CALMING EFFECT ON THE CNS
• SEDATIVES - REDUCES NERVOUSNESS IRRITABILITY
  WITHOUT CAUSING SLEEP
• HYPNOTIC - CAUSES SLEEP

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BARBITUATES

• OVER 50 BARBITUATES APPROVED, ONLY A FEW ARE USED
• BOTH SEDATIVE HYPNOTIC EFFECT
• USED TO CONTROL SEIZURES
• PHENOBARBITAL COMA
• THERAPEUTIC RANGE IN BLOOD

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MEDICATIONS

• ULTRASHORT ACTING - THIOPENTAL
• SHORT ACTING - PENTABARBITAL/NEMBUTAL,
  SECOBARBITAL/SECONAL
• LONG ACTING - PHENOBARBITAL

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SIDE EFFECTS

• BARBITURATES DEPRIVE REM SLEEP
• LEADS TO INABILITY TO HANDLE NORMAL STRESS
• IF BARBITURATES STOPPED, REM SLEEP INCREASES (
  OFTEN NIGHTMARES )
• RESPIRATORY AND MENTAL DEPRESSION

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DRUG INTERACTIONS

• CAUSED BY INCREASED HEPATIC ENZYMES
• LEADS TO INCREASED DRUG METABOLISM BREAKDOWN
• OTHER MEDICATIONS COMPETING FOR SAME ENZYME CAN
  LEAD TO INHIBITED DRUG METABOLISM

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BENZODIAZEPINES

• CLASSIFIED AS EITHER ANXIOLYTICS OR SEDATIVE -
  HYPNOTICS
• HAS A CALMING EFFECT ON THE CNS
• DO NOT SUPPRESS REM SLEEP AS MUCH
• DO NOT INDUCE HEPATIC ENZYME ACTIVITY

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USES

• STOPS SEIZURES
• CONTROLS AGITATION ANXIETY
• INDUCES SLEEP
• SKELETAL MUSCLE RELAXATION
• TREATMENT OF PREVENTION OF DTS
• DEPRESSION
• COMBINED WITH ANESTHETICS

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SIDE EFFECTS

• HA, DROWINESS
• DIZZINESS
• HANGOVER EFFECT
• OVERDOSES RARELY RESULT IN DEATH
• DANGEROUS IF MIXED WITH OTHER CNS DEPRESSANTS OR
  ETOH

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MEDICATIONS

• PROSOM, DALMANE, RESTORIL, HALICON - SLEEP
• CHLORAL HYDRATE
• VALIUM, XANAX, ATIVAN, LIBRIUM, KLONOPIN,
  TRANXENE
• VERSED
• ROMAZICON - antidote

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ANTIDEPRESSANTS
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TRICYCLIC ANTIDEPRESSANTS

• Also treats
• chronic pain associated with Ca
• diabetic neuropathy
• chronic tension HA
• panic disorders
• cocaine withdrawal
• eating disorders

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Side Effects

• anticholinergics effects
• antihistamine effects
• alpha adrenergic effects
• serious life threatening side effects with
  toxicity
• CV

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Medications

• TOFRANIL
• ELAVIL
• SINEQUAN
• PAMELOR

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MOA INHIBITORS

• Used when other medications are not working
• drug-food or drug-drug interactions -
  norepinephrine
• anticholinergic and hepatoxicity side effects

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Medications

• NARDIL
• PARNATE

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SSRI

• Serotonin effects mood, perception of pain,
  sexual function, sleep, appetite
• keeps people balanced
• side effects of anticholinergics, antihistamine
  and alpha adrenergic is less
• has no effect on those receptors

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Medications

• PROZAC
• ZOLOFT
• EFFEXOR
• PAXIL

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MOOD STABILIZERS

• LITHIUM for bipolar

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PHENOTHIAZINES

• Three subgroups - depending on the subgroup will
  have mild to severe of these effects
• strong sedative effects
• hypotensive effects
• anticholinergic effects
• EPS
• bone marrow suppression

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Medications

• THORAZINE
• PROLIXIN
• NAVANE
• HALDOL
• INAPSINE
• COMPAZINE

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DRUG CLOSELY RELATED TO PHENOTHIAZINE

• HALDOL
• less anticholinergic and alpha adrenergic effects
• more prominent EPS
• po, IM, IV

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ANTICONVULSANTS

• NOW CALLED ANTIEPILEPTIC (AED)
• EXACT ACTION NOT KNOWN
• BELIEVE TO ACT DIRECTLY ON ABNORMAL NEURONS
• BY RAISING THE SEIZURE THRESHOLD
• DECREASE NERVE CONDUCTION

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CLASSES

• BENZODIAZEPINES
• KLONOPIN, TRANXENE - CHRONIC
• VALIUM, ATIVAN - ACUTE
• TEGRETOL
• 2ND MOST POPULAR
• INCREASES ITS OWN METABOLISM WITH THE 1ST COUPLE
  OF MONTHS
• PHENOBARBITAL
• VALPROIC ACID - DEPAKOTE

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DILANTIN

• 1ST LINE AED
• BLOOD RANGE
• TOXICITY CAUSES NYSTAGMUS, ATAXIA, ENCEPHALOPATHY
• GINGIVAL HYPERPLASIA, ACNE, HIRSUTISM,
  HYPERTROPHY OF SQ FACIAL TISSUE, OSTEOPEROSIS

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DRUG INTERACTIONS

• HIGHLY BOUND TO PROTEIN SO COMPETES WITH RECEPTOR
  SITES
• INHIBITS HEPATIC ENZYMES
• REMEMBER HOW TO GIVE IV

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MUSCLE RELAXANTS

• Neuromuscular Blocking Agents
• Nondepolarizing
• Depolarizing
• Spasmolytics
• Centrally Acting
• Peripherially Acting
• Benzodiazepine

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Centrally Acting Spasmolytics

• acts specially at the spinal end of the neurons
• does not work on brain related spasms, i.e. CVA
• side effects - CNS, respiratory depression
• BACLOFEN
• FLEXERIL
• SOMA
• ROBAXIN

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Peripherally Acting Spasmolytics

• acts directly on the muscle
• used for spinal cord injuries, MS, CP, CVA
• side effects- depresses all muscles which leads
  to
• DANTRIUM

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MOVEMENT DISORDERS

• Parkinson
• Treat by increasing dopamine or lowering
  acetylcholine
• look at pg 386

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Dopaminergics

• Combining with Carbidopa inhibits peripheral
  destruction of the Levodopa
• half life 1-2 hours with duration 5 hours
• multiple side effects
• SINEMET
• SYMMETREL
• PARLODEL

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Anticholinergics

• blocks the access of acetylcholine to cholinergic
  receptors
• less effective than the dopaminergics
• think of side effects of anticholinergics
• COGENTIN
• BENEDRYL
• ARTANE

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REVIEW THESE MEDICATIONS

• CARDIAC GLYCOSIDES
• DIGOXIN
• ANTIDYSRHYTHMIC AGENTS
• CLASS Ia, Ib, Ic, CLASS II (BETA BLOCKERS), CLASS
  III, CLASS IV (CALCIUM CHANNEL BLOCKERS
• ANTIANGINAL AGENTS
• NITRATES, CALCIUM CHANNEL BLOCKERS, BETA BLOCKERS

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ANTICOAGULATION MEDICATIONS

• HEPARIN
• COUMADIN
• ANTIPLATLET INHIBITORS
• ASA, PLAVIX, TICLID, INTEGRILIN, PERSANTINE
• ANTITHROMBOLYTICS
• TPA, RETAVASE, STREPTOKINASE

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MEDICATIONS THAT EFFECT THE RESPIRTORY SYSTEM

• BRONCODILATORS
• XANTHINES
• CAFFEINE, THEOPHYLLINE, THEODUR, ELIXOPHYLLIN,
  SLO-BID, THEO-24, UNIPHYL
• BETA 2 AGONISTS
• ALBUTEROL, MAXAIR, SEREVENT, BRETHINE
• BETA 1 2
• ISUPREL, ALUPENT, METAPREL

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BRONCHODILATORS

• ALPHA BETA
• EPINEPHRINE (TO INCLUDE MANY OTC INHALERS),
  EPHEDRINE

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OTHER RESPIRATORY AGENTS

• ANTICHOLINERGICS - PREVENTS BRONCHOCONSTRICTION
• ACTIONS ARE SLOW PROLONGED
• ATROVENT
• CORTICOSTEROIDS
• INHALERS - BECLOVENT, VANCERIL, AEROBID, AZMACORT
• MAST CELL STABILIZERS
• CROMOLYN/INTAL, TILADE

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OTHER RESPIRATORY MEDS

• DECONGESTANTS
• ANTITUSSIVES
• EXPECTORANTS
• ANTIHISTAMINES
• MUCOLYTICS
• MYCOMYST

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ANTIHYPERTENSIVE AGENTS

• DIURETICS
• ADRENERGIC BLOCKERS
• VASODILATORS
• ACE INHIBITORS
• CALCIUM CHANNEL BLOCKERS
• DIRECT PERIPHERALLY ACTING AGENTS

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ANTILIPEMIC AGENTS

• BILE ACID SEQUESTRANTS
• QUESTRAN
• HMG-CoA REDUCTASE INHIBITORS
• MEVACOR, ZOCOR, PRAVACHOL, LESCOL, LIPITOR
• FIBRIC ACID DERIVATIVES
• NICOTINIC ACID
• NIACIN

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DIURETICS

• LOOP DIURETICS
• LASIX, DEMEDEX
• OSMOTIC DIURETICS
• MANNITOL
• POTASSIUM SPARING
• ALDACTONE
• THIAZIDES - HCTZ
• CARBONIC ANHYDRASE- DIAMOX

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UPPER GI DRUGS

• ANTACIDS
• H2 BLOCKERS
• PROTON PUMP INHIBITORS
• GI STIMULANT
• ANTEMETICS
• ANTIPSYCHOTICS, ANTICHOLINERGICS, ANTIHISTAMINE
• EMETIC
• IPECAC

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LOWER GI DRUGS

• ANTIFLATULANTS
• SIMETHICONE
• ANTIDIARRHEALS
• ATROPINE BASED
• OPIATES
• LAXATIVES
• SALINE, BULK FORMING,LUBRICANT, SURFACTANTS,
  STIMULANTS

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GLUCOCORTICOIDS

• USES
• MULTIPLE SIDE EFFECTS
• PREDNISONE
• DECADRON
• SOLUMEDROL

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THYROID AGENTS

• Hypothyroid
• LEVOTHYROXINE
• SYNTHROID
• Hyperthyroid
• TAPAZOLE PTU - Blocks the use of iodine

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ANTIDIABETIC HYPOGLYCEMIC AGENTS

• INSULIN
• REGULAR - SHORT ACTING
• NPH LENTE - INTERMEDIATE
• ULTRALENTE - LONG
• HUMALOG
• FIXED COMBINATION

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ORAL AGENTS

• 2 GENERATIONS OF SULFONYLUREA
• DIABINESE - FIRST GENERATION
• ELIMINATES IN KIDNEYS
• FACIAL FLUSHING IF TAKEN WITH ETOH

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SECOND GENERATION

• GLUCOTROL, DIABETA, MICRONASE, GLYNASE
• MORE POTENT RAPID ONSET
• NOT CONTAINDICATED WITH RENAL FAILURE

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IMMUNOSUPPRESSANT AGENTS

• SUPPRESS CERTAIN LYMPHOCYTE CELL LINES,
  PREVENTING THE IMMUNE RESPONSE INVOLVEMENT
• IMURAN - RENAL TRANSPLANTS ARTHRITIS
• CYCLOSPORIN A - LIVER, KIDNEY HEART
  TRANSPLANTS, ARTHRITIS, IBS, PSORIASIS

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SIDE EFFECTS

• IMURAN
• IMMUNOSUPPRESSION, LEUKOPENIA
• CYCLOSPORIN A
• NEPRO/HEPATOTOXICITY, HTN

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ANTINEOPLASTICS

• CCNS - DRUGS THAT ARE CYTOTOXIC IN ANY PHASE OF
  CELL MITOSIS
• USED ON LARGE, SLOW GROWING TUMORS
• CCS - DRUGS THAT ARE CYTOTXIC AT A SPECIFIC PHASE
  OF CELL MITOSIS
• USED ON RAPID GROWING TUMORS

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ACTION

• COMBINATION THERAPY
• EFFECTIVE ON THAT TYPE OF CANCER
• HAVE DIFFERENT MECHANISMS OF ACTION
• POSSESS DIFFERENT CYTOTOXIC PROPERTIES

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SIDE EFFECTS

• HARMFUL TO RAPID GROWING CELLS
• ALOPECIA, GI DISTURBANCES, BONE MARROW
  SUPPRESSION
• DOSE LIMITING SIDE EFFECTS
• EMETIC POTENTIAL

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ALKYLATING AGENTS

• MUSTARD GAS THE DERIVATIVES OF THE NITROGEN
  MUSTARDS
• CCNS
• COMBINATION THERAPY
• CAUSE DOSE LIMITING SIDE EFFECTS
• EXTRAVASATION

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MEDICATIONS

• NITROGEN MUSTARD/MUSTARGEN
• CYTOXAN
• CISPLATIN

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ANTIMETABOLITES

• MIMICS THE ACTIONS OF IMPORTANT PRECURSORS NEEDED
  FOR DNA RNA SYNTHESIS
• FALSELY USES PURINES, PYRIMIDINES OR FOLIC ACID
• INHIBITS CRITICAL ENZYMES
• CCS
• COMBINATION, HEMATOLOGIC SOLID TUMORS

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MEDICATIONS

• METHOTREXATE
• MERCAPTOPURINE/6-MP
• CYTOSAR
• LEUCOVORIN RESCUE - USED TO REVERSE METHOTREXATE
  TOXICITIY

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CYTOTOXIC ANTIBIOTICS

• TOO TOXIC FOR INFECTIONS
• CCNS
• COMBINATION, HEMATOLOGIC SOLID TUMORS

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MEDICATIONS

• ADRIAMYCIN
• BLEOMYCIN

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MITOTIC INHIBITORS

• AFFECT THE CELL CYCLE SHORTLY BEFORE OR DURING
  MITOSIS
• CCS

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MEDICATIONS

• TAXOL
• VINCRISTINE
• VINBLASTINE

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MISCELLANOUS ANTINEOPLASTICS

• HEXALEN
• ELSPAR
• HYDREA

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NSAIDS

• WORKS FROM THE ABILITY TO INHIBIT THE ARACHIDONIC
  ACID PATHWAY, PREVENTING THE RELEASE OF
  PROSTAGLADINS LEUKOTRIENES
• USED FOR ANALGESIC, ANTIGOUT, ANTIINFLAMMATORY,
  ANTIPYRETIC, VASCULAR HEADACHES PLATLET
  INHIBITION

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SIDE EFFECTS

• GI - HEARTBURN, NAUSEA, GI BLEED
• RENAL - REDUCTION OF CREATININE CLEARANCE
• HEPATIC - TOXICITY
• OTHER - SENSITIVITY, TINNITUS, HEARING LOSS

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MEDICATIONS

• VOLTAREN, LODINE, INDOCIN, TOLECTIN
• ASA, DOLOBID
• NALFON, ANSAID, MOTRIN, ORUDIS, TORADOL,
  NAPROSYN, DAYPRO
• FELDENE
• RELAFEN

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ANTIGOUT

• ZYLOPRIN/ALLOPURINAL - PREVENTS URIC ACID
  PRODUCTION
• COLCHINE - REDUCES THE INFLAMMATORY RESPONSE OF
  THE URATE CRYSTALS IN THE JOINT
• PROBENECID - INCREASES THE EXCRETION OF URIC ACID

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ANTIBIOTICS

• SULFONAMIDES
• BACTRIM, PEDIZOLE, SEPTRA
• PENICILLINS
• 4 CLASSIFICATIONS COMBINATION DRUGS
• LITTLE EFFECT ON GRAM NEGATIVE BACTERIA
• GENERALLY MEDICATIONS THAT END IN CILLIN

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CEPHALOSPORINS

• STRUCTURALLY LIKE PCN
• CROSS SENSITIVITY
• DIFFERENT GENERATIONS WORK BETTER ON GRAM
  POSITIVE OR NEGATIVE
• ANCEF, KEFLEX, MEFOXIN, CEFTIN/ZINACEF, SUPRAX,
  ROCEPHIN, FORTAZ

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TETRACYCLINES

• STRONG AFFINITY FOR CALCIUM
• GRAM POSITIVE NEGATIVE
• CAUSE DISCOLORATION OF ENAMEL RETARD FETAL
  SKELETAL DEVELOPMENT
• DOXYCYCLINE

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AMINOGLYCOSIDES

• VERY POTENT
• GRAM NEGATIVE POSITIVE
• OTOTOXICITY NEPHROTOXICITY - FOLLOW PEAKS
  TROUGHS
• AMIKIN, GENTAMYCIN, NEOMYCIN, STREPTOMYCIN,
  TOBRAMYCIN

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QUINOLONES/FLUOROQUINOLONES

• POTENT BROAD SPECTRUM
• NOT USED IN CHILDREN - SUPPRESSES LAB ANIMAL
  GROWTH
• CIPRO, FLOXIN

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MACROLIDES

• WIDED VARIETY OF INFECTIONS
• ERTHROMYCIN (SALTS), ZITHROMAX, BIAXIN
• MISCELLANEOUS ANTIBIOTICS
• CLINDAMYCIN
• PRIMAXIN
• VANCOMYCIN - TREATS MRSA, SIMILAR TO
  AMINOGLYCOSIDES (NEEDS BLOOD LEVELS MONITORED)

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ANTITUBERCULAR AGENTS

• DIVIDED INTO 2 GROUPS
• FIRST LINE - ETHAMBUTOL, ISONIAZID (INH),
  PYRAZINAMIDE (PZA), RIFAMPIN, STREPTOMYCIN
• SECOND LINE
• INH, PZA, RIFAMPIN, STREPTOMYCIN - MONITOR LIVER
• RIFAMPIN - DISCOLORS