Pharmacology Overview Part II

1. Pharmacology Overview Part II Becca Maddox NURS 2205 March 27, 2002

2. 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

3. 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

4. AMPHETAMINES MOOD ELEVATION, INCREASE MENTAL ALERTNESS, DECREASED FATIGUE & DROWINESS USED TO TREAT NARCOLEPSY & ADD HIGH RECREATIONAL ABUSE

5. 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

6. ANOREXIANTS SUPPRESSES APPETITES DIDREX PHENYLPROPANOLAMINE (DEXATRIM, ACUTRIM)

7. TREATMENT OF ADD DEXTROAMPHETAMINE / AMPHETAMINES RITALIN Has the opposite effect, not understood

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

9. ANOREXIANT / AMPHETAMINE TALK ABOUT AS A CNS STIMULANT BUT IS AN INDIRECT ALPHA AGONIST

10. CNS DEPRESSANTS

11. 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

12. MEDICATIONS (INHALANTS) ISOFLURANE HALOTHANE ENFLURANE NITROUS OXIDE - LAUGHING GAS

13. 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

14. LOCAL ANESTHESIA COMES IN MANY FORMS �CAINES� LIDOCAINE, CARBOCAINE, NOVACAIN, PONTOCAINE SQ INJECTIONS WITH & WITHOUT EPINEPHRINE MIXED WITH IM ANTIBIOTICS

15. 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

16. NARCOTIC ANALGESIC CLASSIFIED BY THEIR MECHANISM OF ACTION OR BY CHEMICAL MAKEUP CHEMICAL STRUCTURE - OPIATES MECHANISM OF ACTION - AGONIST, AGONIST-ANTAGONIST, PARTIAL AGONIST

17. 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

18. 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

19. SIDE EFFECTS NAUSEA & VOMITING PATIENTS OFTEN CONFUSE THE HISTAMINE RESPONSE AS AN ALLERGIC REACTION OPIOID TOLERANCE PHYSICAL DEPENDENCE

20. THERAPEUTIC USES RELIEVE MODERATE TO SEVERE PAIN CONTROL DIARRHEA SUPPRESS COUGHING MAINTAIN BALANCED ANESTHESIA

21. 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

22. MEDICATIONS MORPHINE, MS CONTIN CODEINE DEMEROL METHADONE DILAUDID FENTANYL, DURAGESIC OXYCODONE PROPOXYPHENE

23. AGONIST-ANTAGONIST TALWIN NUBAIN STADOL

24. COMBINATIONS DARVOCET/WYGESIC, DARVON TYLENOL #3 FIORINAL, FLORICET LORCET/VICODIN, LORTAB PERCOCET/TYLOX, PERCODAN ROXICET

25. SEDATIVE-HYPNOTICS AGENTS HAS A CALMING EFFECT ON THE CNS SEDATIVES - REDUCES NERVOUSNESS & IRRITABILITY WITHOUT CAUSING SLEEP HYPNOTIC - CAUSES SLEEP

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

27. MEDICATIONS ULTRASHORT ACTING - THIOPENTAL SHORT ACTING - PENTABARBITAL/NEMBUTAL, SECOBARBITAL/SECONAL LONG ACTING - PHENOBARBITAL

28. 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

29. 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

30. 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

31. USES STOPS SEIZURES CONTROLS AGITATION & ANXIETY INDUCES SLEEP SKELETAL MUSCLE RELAXATION TREATMENT OF & PREVENTION OF DT�S DEPRESSION COMBINED WITH ANESTHETICS

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

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

34. ANTIDEPRESSANTS

35. TRICYCLIC ANTIDEPRESSANTS Also treats chronic pain associated with Ca diabetic neuropathy chronic tension HA panic disorders cocaine withdrawal eating disorders

36. Side Effects anticholinergics effects antihistamine effects alpha adrenergic effects serious life threatening side effects with toxicity CV

37. Medications TOFRANIL ELAVIL SINEQUAN PAMELOR

38. MOA INHIBITORS Used when other medications are not working drug-food or drug-drug interactions - norepinephrine anticholinergic and hepatoxicity side effects

39. Medications NARDIL PARNATE

40. 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

41. Medications PROZAC ZOLOFT EFFEXOR PAXIL

42. MOOD STABILIZERS LITHIUM for bipolar

43. 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

44. Medications THORAZINE PROLIXIN NAVANE HALDOL INAPSINE COMPAZINE

45. DRUG CLOSELY RELATED TO PHENOTHIAZINE HALDOL less anticholinergic and alpha adrenergic effects more prominent EPS po, IM, IV

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

47. 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

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

49. DRUG INTERACTIONS HIGHLY BOUND TO PROTEIN SO COMPETES WITH RECEPTOR SITES INHIBITS HEPATIC ENZYMES REMEMBER HOW TO GIVE IV

50. MUSCLE RELAXANTS Neuromuscular Blocking Agents Nondepolarizing Depolarizing Spasmolytics Centrally Acting Peripherially Acting Benzodiazepine

51. 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

52. 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

53. MOVEMENT DISORDERS Parkinson Treat by increasing dopamine or lowering acetylcholine look at pg 386

54. 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

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

56. 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

57. ANTICOAGULATION MEDICATIONS HEPARIN COUMADIN ANTIPLATLET INHIBITORS ASA, PLAVIX, TICLID, INTEGRILIN, PERSANTINE ANTITHROMBOLYTICS TPA, RETAVASE, STREPTOKINASE

58. 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

59. BRONCHODILATORS ALPHA & BETA EPINEPHRINE (TO INCLUDE MANY OTC INHALERS), EPHEDRINE

60. OTHER RESPIRATORY AGENTS ANTICHOLINERGICS - PREVENTS BRONCHOCONSTRICTION ACTIONS ARE SLOW & PROLONGED ATROVENT CORTICOSTEROIDS INHALERS - BECLOVENT, VANCERIL, AEROBID, AZMACORT MAST CELL STABILIZERS CROMOLYN/INTAL, TILADE

61. OTHER RESPIRATORY MEDS DECONGESTANTS ANTITUSSIVES EXPECTORANTS ANTIHISTAMINES MUCOLYTICS MYCOMYST

62. ANTIHYPERTENSIVE AGENTS DIURETICS ADRENERGIC BLOCKERS VASODILATORS ACE INHIBITORS CALCIUM CHANNEL BLOCKERS DIRECT & PERIPHERALLY ACTING AGENTS

63. ANTILIPEMIC AGENTS BILE ACID SEQUESTRANTS QUESTRAN HMG-CoA REDUCTASE INHIBITORS MEVACOR, ZOCOR, PRAVACHOL, LESCOL, LIPITOR FIBRIC ACID DERIVATIVES NICOTINIC ACID NIACIN

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

65. UPPER GI DRUGS ANTACIDS H2 BLOCKERS PROTON PUMP INHIBITORS GI STIMULANT ANTEMETICS ANTIPSYCHOTICS, ANTICHOLINERGICS, ANTIHISTAMINE EMETIC IPECAC

66. LOWER GI DRUGS ANTIFLATULANTS SIMETHICONE ANTIDIARRHEALS ATROPINE BASED OPIATES LAXATIVES SALINE, BULK FORMING,LUBRICANT, SURFACTANTS, STIMULANTS

67. GLUCOCORTICOIDS USES MULTIPLE SIDE EFFECTS PREDNISONE DECADRON SOLUMEDROL

68. THYROID AGENTS Hypothyroid LEVOTHYROXINE SYNTHROID Hyperthyroid TAPAZOLE & PTU - Blocks the use of iodine

69. ANTIDIABETIC & HYPOGLYCEMIC AGENTS INSULIN REGULAR - SHORT ACTING NPH & LENTE - INTERMEDIATE ULTRALENTE - LONG HUMALOG FIXED COMBINATION

70. ORAL AGENTS 2 GENERATIONS OF SULFONYLUREA DIABINESE - FIRST GENERATION ELIMINATES IN KIDNEYS FACIAL FLUSHING IF TAKEN WITH ETOH

71. SECOND GENERATION GLUCOTROL, DIABETA, MICRONASE, GLYNASE MORE POTENT & RAPID ONSET NOT CONTAINDICATED WITH RENAL FAILURE

72. 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

73. SIDE EFFECTS IMURAN IMMUNOSUPPRESSION, LEUKOPENIA CYCLOSPORIN A NEPRO/HEPATOTOXICITY, HTN

74. 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

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

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

77. ALKYLATING AGENTS MUSTARD GAS & THE DERIVATIVES OF THE NITROGEN MUSTARDS CCNS COMBINATION THERAPY CAUSE DOSE LIMITING SIDE EFFECTS EXTRAVASATION

78. MEDICATIONS NITROGEN MUSTARD/MUSTARGEN CYTOXAN CISPLATIN

79. 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

80. MEDICATIONS METHOTREXATE MERCAPTOPURINE/6-MP CYTOSAR LEUCOVORIN RESCUE - USED TO REVERSE METHOTREXATE TOXICITIY

81. CYTOTOXIC ANTIBIOTICS TOO TOXIC FOR INFECTIONS CCNS COMBINATION, HEMATOLOGIC & SOLID TUMORS

82. MEDICATIONS ADRIAMYCIN BLEOMYCIN

83. MITOTIC INHIBITORS AFFECT THE CELL CYCLE SHORTLY BEFORE OR DURING MITOSIS CCS

84. MEDICATIONS TAXOL VINCRISTINE VINBLASTINE

85. MISCELLANOUS ANTINEOPLASTICS HEXALEN ELSPAR HYDREA

86. 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

87. SIDE EFFECTS GI - HEARTBURN, NAUSEA, GI BLEED RENAL - REDUCTION OF CREATININE CLEARANCE HEPATIC - TOXICITY OTHER - SENSITIVITY, TINNITUS, HEARING LOSS

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

89. 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

90. ANTIBIOTICS SULFONAMIDES BACTRIM, PEDIZOLE, SEPTRA PENICILLINS 4 CLASSIFICATIONS & COMBINATION DRUGS LITTLE EFFECT ON GRAM NEGATIVE BACTERIA GENERALLY MEDICATIONS THAT END IN �CILLIN�

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

92. TETRACYCLINES STRONG AFFINITY FOR CALCIUM GRAM POSITIVE & NEGATIVE CAUSE DISCOLORATION OF ENAMEL & RETARD FETAL SKELETAL DEVELOPMENT DOXYCYCLINE

93. AMINOGLYCOSIDES VERY POTENT GRAM NEGATIVE & POSITIVE OTOTOXICITY & NEPHROTOXICITY - FOLLOW PEAKS & TROUGHS AMIKIN, GENTAMYCIN, NEOMYCIN, STREPTOMYCIN, TOBRAMYCIN

94. QUINOLONES/FLUOROQUINOLONES POTENT BROAD SPECTRUM NOT USED IN CHILDREN - SUPPRESSES LAB ANIMAL GROWTH CIPRO, FLOXIN

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

96. 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