Pharmacology Exit Exam Study Notes PDF

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Pharmacology Exit Exam Study Notes Pharmaceutics  The study of how various drug forms influence the way the drug affects the body  Helps to inform choice of route of administration  Pharmacokinetics  The study of what the body does to the drug  Pharmacodynamics  The study of what the drug does to the body Analgesics  Medications that relieve pain without causing loss of consciousness  “Painkillers”  Opioid analgesics  Adjuvant analgesic drugs Adjuvant Drugs  Assist primary drugs in relieving pain Opioid Analgesics  Three classes base on their mechanisms of action:  Agonists: bind to opioid pain receptor in the brain to reduce pain  Agonists-antagonists: bind to a pain receptor, causing a weaker response than full agonists  Antagonists (non-analgesic): bind to a pain receptor and exert no response  reverse the effects of agonist drugs on pain receptors (competitive binding)  Prototype: Morphine Sulphate Nonopioid Analgesics  Prototype: acetaminophen (Tylenol) Opioid Antagonist: Naloxone 

Central Nervous System Depressants  Sedatives: drugs that have an inhibitory effect on the CNS system to the degree that they reduce nervousness, excitability and irritability  Hypnotics: cause sleep Benzodiazepines  Formerly the most commonly prescribed sedative-hypnotic drugs  Prototype: diazepam (Valium) Nonbenzodiazepines  Zopiclone (Imovane)  Short-acting benzo-like drug  Very short half life  Short-term treatment of insomnia (7-10 days) Barbiturates  First introduced in early 1900’s and were the standard for insomnia and sedation  Habit forming; low therapeutic index

 Only a few commonly used today due to safety and efficacy of benzodiazepines  Prototype: phenobarbital OTC Hypnotics  Nonprescription sleeping aids often contain antihistamines, which have a CNS-depressant effect  I.e.. diphenhydramine Muscle Relaxants  Act to relieve pain associated with skeletal muscle spasms  Most of centrally acting  Similar in action of other CNS depressants  Direct acting  Act directly on skeletal muscle  Prototype: baclofen (Lioresal) Drugs to treat adhd: amphetamines  Prototype: methylphenidate (Ritalin, concerta) Anxiolytics: benzodiazepines  Prototype: diazepam (valium)  See content from week 5 as it is the same  Lorazepam (Ativan)  Intermediate-acting benzodiazepine  Can be given IV or IM; useful in treatment of acutely agitated patients  Also used to treat or prevent alcohol withdrawal Mood-stabilizing drugs  Lithium  Antidepressants Mood-stabilizers: antidepressants  First generation:  Tricyclics  Tetracyclic  MAOIs  Second generation  SSRIs  Serotonin-norepinephrine reuptake inhibitors (SNRIs)  miscellaneous  Tricyclic Antidepressants  Have largely been replaced by SSRIs as first line antidepressant drugs (still considered second line drugs)  Can be used as adjunct to newer-generation antidepressants  Mechanism of action: block reuptake of neurotransmitters causing accumulation at the nerve endings  It is thought they may help regulate malfunctioning neurons  Serotonin-selective reuptake inhibitors (ssris)  Second-generation antidepressants  Prototype: fluoxetine (Prozac)

Mechanism of action:  inhibit reuptake of serotonin from CNS synapses to increase Antipsychotics  Drugs used to treat mental illness  Prototype: risperidone (risperidal)  Atypical antipsychotic Antipsychotics: Risperidone (Risperdal)  used specifically for schizophrenia (including negative symptoms)  Minimal eps at therapeutic dosages  Oral and long-acting injectable forms Antibiotics  Used to treat BACTERIAL infections Antibiotic Therapy  Empiric therapy  Treatment BEFORE specific culture information has been reported or obtained  Definitive therapy  Treatment tailored to treat organism identified with cultures  Prophylactic therapy  Treatment to PREVENT an infection  Therapeutic response  Decrease in specific signs and symptoms of infection  Such as?  Subtherapeutic response  Signs and symptoms of infection do not improve  Allergic reactions  Penicillin and sulfonamides are two broad classes of antibiotics to which many people have allergic anaphylactic reactions Actions of Antibiotics  Bactericidal  Kill the bacteria  Bacteriostatic  Inhibit growth, eventually leads to bacterial death Classes of Antibiotics  Sulfonamides  Penicillin  Cephalosporins  Carbapenems  Macrolides  Quinolones  Aminoglycosides  Tetracyclines Sulfonamides  One of the first groups of antibiotics  Often combined with another antibiotic 

Prototype: sulfamethoxazole  often used in combo with trimethoprim to make SMX-TMP (Septra) Penicillin  Various types of penicillin  Natural penicillin:  penicillin G, penicillin V  Penicillinase-resistant drugs:  cloxacillin sodium  Aminopenicillins:  amoxicillin, ampicillin  Extended-spectrum:  piperacillin sodium/tazobactam sodium  Prototype: Penicillin V Cephalosporins  Synthetic antibiotics  Structurally and pharmacologically related to penicillin  Bactericidal  Broad spectrum  Divided into groups according to their antimicrobial activity  Prototypes:  Cefazolin (Ancef)  Ceftriaxone (Rocephin)  Adverse effects:  Similar to those of penicillin  Mild diarrhea, abdominal cramping, rash, pruritus, redness, edema  Potential cross-sensitivity with penicillin if allergies exist Cephalosporins: Cefazolin  First generation cephalosporin  Available parenterally (IV or IM)  Good grade-positive coverage, poor gram-negative coverage  Uses:  Surgical prophylaxis  Susceptible staphylococcal infections 

Cephalosporins: Ceftriaxone  Third generation cephalosporin  Most potent group against gram-negative bacteria, less active against gram-positive bacteria  Given parenterally (IV or IM)  Uses:  Any susceptible bacteria Macrolides  Prototype: Azithromycin (Zithromax)  Mechanism of action:

 Bacteriostatic: prevent protein synthesis within bacterial cells Tetracyclines  Prototype: doxycycline (Doxycin)  Mechanism of action:  Bacteriostatic: inhibit bacterial growth and bacterial protein synthesis Nonsteroidal Anti-inflammatory Drugs (NSAIDs)  A large and chemically diverse group of drugs that have these properties:  Analgesic  Anti-inflammatory  Antipyretic  **ASA (Aspirin) also has anti-platelet properties NSAIDs by class  Salicylates  Acetylsalicylic Acid (ASA) (Aspirin)  Acetic Acid derivatives  Ketorolac (Toradol)  Cyclo-oxygenase (COX)-2 inhibitors  Celecoxib (Celebrex)  Propionic acid derivatives  Ibuprofen (Advil), naproxen (Naprosyn) Salicylate Anti-inflammatory durgs  Prototype: Acetylsalicylic Acid (Aspirin)  Aka ASA  Mechanism of action:  Irreversibly binds to COX-1 receptors within the platelets  Reduced formation of clotting factors that normally promote platelet aggregation (clotting) Acetic Acid Derivatives  Prototype: ketorolac (Toradol)  Uses:  Some anti-inflammatory effect but primarily used for analgesic effects  Comparable to narcotics for effect  Short term use (5 to 7 days) for moderate to severe acute pain (ie. Post-op, postpartum) Propionic acid derivatives  Prototype: ibuprofen (Advil, Motrin)  Most commonly used NSAID COX-2 inihibitor  Prototype: celecoxib (Celebrex)  First and only COX-2 inhibitor Antigout Drugs  Prototype: allopurinol (Zyloprim)  Mechanism of action:  Inhibits canthine oxidase to prevent uric acid production

 Prototype: colchicine Antiviral Drugs  Antiviral drugs  Used to treat infections caused by viruses other than HIV  Antiretroviral drugs  Used to treat infections caused by HIV, the virus that causes AIDS Herpes Simples and Varicella-Zoster Virus Infections  Acyclovir may speed recovery; best results are generally seen when antiviral medication is started within 72 hrs of symptom onset  Zostavax Antiviral Drugs (Non-HIV)  Prototype: Acyclovir (Zovirax)  Synthetic nucleoside analogue  Used to suppress replication of HSV1, HSV2 and VZV  Medication of choice for treatment of initial and recurrent episodes of these infections  Given orally, topically or parenterally  Prototype: Oseltamivir phosphate (Tamiflu)  Neuraminidase inhibitior  Active against influenza types A and B  Reduce duration of illness  Treatment should begin within 2 days of influenza symptom onset  Given orally Antiretroviral Drugs  Highly active antiretroviral therapy  Includes at least 3 medications that each work in different ways to reduce the viral load  Reverse transcriptase inhibitors  Block activity of reverse transcriptase enzymes, preventing production of new viral DNA  Protease inhibitors  Inhibit the protease retroviral enzyme, preventing viral replication  Fusion inhibitor  Inhibit viral fusion, preventing viral replication  Entry inhibitor  CCR5 co-receptor anatagonists (CCR5 is used as an entry point into the cell)  Integrase inhibitors  Inhibit integrase enzyme, preventing intergration of the viral gene into human DNA Antiretroviral Prototype: enfuvirtide (Fuzeon)  Fusion inhibitor Acid-Controlling Drugs  Antacids

 H2 Antagonists  Proton Pump Inhibitors Antacids  Basic compounds used to neutralize stomach acid  Salts of aluminum, magnesium, calcium or sodium bicarb  Many antacids also contain simethicone  Magnesium added to aluminum and calcium based formulations Histamine Receptor Antagonists  Reduce acid secretion  All available OTC in lower-dosage forms  Most popular drugs for treatment of acid-related disorders  Prototype: ranitidine hydrochloride (Zantac) Proton Pump Inhibitors  Review: parietal cells release H+ ions (protons) during hydrochloric acid production  the proton pump  H2 blockers and histamines do not stop the action of the pump  Prototype: omeprazole (Losec) Simethicone (Ovol)  Anti-flatulent drug used to reduce discomfort of gastric/intestinal gas  Can be used in combo with antacids  Often in combo with calcium carbonate  Alters elasticity of mucus-coated gas bubbles to break them down into smaller ones  Decreased gas pain and increased expulsion via mouth or rectum Antidiarrheals  Adsorbents  Antimotility drugs  Anticholinergics  Opiates  Probiotics (aka intestinal flora modifiers and bacterial replacement drugs Antidiarrheals: Adsorbents  Prototype: bismuth subsalicylate (Pepto-Bismol)  Mechanism of Action  Coat the walls of the GI tract  Bind to causative bacteria/toxin, which is then eliminated through the stool Antidiarrheals: Antimotility  Prototype: atropine  Anticholinergics: Mechanism of Action  Decreased intestinal tone and peristalsis  Slows movement of fecal matter through GI tract  Have a drying effect  Reduce gastric secretions  Opiates Adverse Effects  Drowsiness, dizziness, lethargy,  N/V, constipation

 Respiratory depression, Hypotension  Urinary retention  Flushing  Prototype: diphenoxylate hydrochloride with atropine sulphate Antidiarrheals: Probiotics  Also known as intestinal flora modifiers and bacterial replacement drugs  Prototype: Lactobacillus acidophilus Laxatives  Bulk forming  Emollient (stool softeners, lubricant laxatives)  Hyperosmotic  Saline  Stimulant Laxatives: Bulk Forming  Prototype: psyllium (Metamucil)  Mechanism of Action  High fiber  Absorb water to increase bulk  Distend the bowel to initiate reflex bowel activity Laxatives: Emollient  Prototype: docusate sodium (Colace)- stool softener  Mechanism of Action  Stool softeners and lubricants  Promote more water and fat in the stools  Lubricate fecal material and intestinal wall Laxatives: Hyperosmotics  Prototypes: Polyethylene glycol  Mechanism of Action  Increase fecal water content  Results in bowel distention, increased peristalsis and evacuation Laxatives: Saline  Prototype: magnesium hydroxide (MOM)  Mechanism of Action  Increases osmotic pressure in the intestinal tract, causing more water to enter the intestines  Bowel distention, increased peristalsis and evacuation Laxatives: Stimulants  Prototype: senna (Senokot)  Mechanism of Action  Increase peristalsis by intestinal nerve stimulation Antihistamine drugs (h1 receptor blockers)  Prototype: dimenhydrinate (Gravol)  Mechanism of action:  Competitive binding to H1 receptors to inhibit acetylcholine binding

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Inhibit cholinergic stimulation in vestibular and reticular areas to prevent nausea and vomiting

Uses:  Motion sickness, nonproductive cough, allergy symptoms, sedation Antidopaminergic drugs  Prototype: prochlorperazine (Proclorazine)  Mechanism of Action:  block dopamine receptors in the CTZ  Uses:  GERD, delayed gastric emptying Serotonin blockers  Prototype: ondansetron (Zofran)  Mechanism of action:  Block serotonin receptors in the GI tract, CTZ and vomiting center  Uses:  For N/V in patients receiving chemotherapy  Postoperative N/V Tetrahydro cannabinoids (THC)  Mechanism of Action:  Major psychoactive substance in marijuana  Inhibitory effects on reticular formation, thalamus, and cerebral cortex to alter mood and body’s perception of its surroundings, which may help relieve N/V  Uses:  Used for N/V associated with chemotherapy and for anorexia associated with weight loss in AIDS patients 

Miscellaneous Anti-nausea drugs  Doxylamine succinate (Diclectin)  Antihistamine  Provided anti-nausea and antiemetic effects in pregnancy  Needs to be tapered down when discontinuing Herbal products: ginger  Used for nausea and vomiting, including that caused by chemo, morning sickness and motion sickness  Adverse effects:  Anorexia, N/V, skin reactions  Drug interactions:  May increase absorption of oral medications  Increase bleeding risk with anticoagulants DEFINITIONS  GLYCONEOGNESIS:  FORMATION OF GLYCOGEN FROM NON-CARBOHYDRATE SOURCES  GLUCOSE:  BASIC, SIMPLE SUGAR

GLYCOGEN:  POLYSACCHARIDE STORED FOR LATER USE  GLYCOGENOLYSIS:  BREAKDOWN OF GLYCOGEN INTO GLUCOSE  GLYCOGENESIS:  PROCESS THAT CONVERTS CARBOHYDRATES INTO GLYCOGEN (STIMULATED BY INSULIN) Nonpharmacological treatment interventions  TYPE 1:  ALWAYS REQUIRES INSULIN THERAPY  TYPE 2:  WEIGHT LOSS  SMOKING CESSAITON  IMPROVED DIETARY HABITS  REDUCED ALCOHOL CONSUMPTION  REGULAR PHYSICAL EXERCISE Types of antidiabetic drugs  INSULINS  ORAL HYPOGLYCEMIC DRUGS  A COMBINATION OF ANTIHYPERGLYCEMIC AND INSULIN CONTROLS GLUCOSE LEVELS INSULIN  FUNCTION AS A SUBSTITUE FOR THE ENDOGENOUS HORMONE  EFFECTS ARE THE SAME AS THOSE OF NORMAL ENDOGENOUS INSULIN  RESTORES THE PATIENT’S ABILITY TO:  METABOLIZE CARBOHYDRATES, FATS AND PROTEINS  STORE GLUCOSE IN THE LIVER  CONVERT GLYCOGEN TO FAT STORES  TYPES OF INSULIN:  RAPID-ACTING:  ASPART (NOVORAPID), LISPRO (HUMALOG)  REGULAR/SHORT-ACTING:  HUMULIN-R  INTERMEDIATE-ACTING:  NPH (HUMULIN N)  LONG-ACTING:  DETERMIR (LEVEMIR), GLARGINE (LANTUS) SHORT-ACTING INSULINS  REGULAR INSULIN (HUMULIN-R, NOVOLIN TORONTO)  ROUTES OF ADMINISTRATION: IV (BOLUS OR INFUSION), IM OR SUBCUT  ONSET (SC): 30 MINUTES  PEAK (SC): 2-3 HOURS  DURATION (SC): 6.5 HOURS  WORKS BEST WHEN GIVEN ABOUT 30MIN BEFORE MEALS INTERMEDIATE-ACTING INSULIN 

 INSULIN ISOHPANE SUSPENSION (NPH)  CLOUDY APPEARANCE  OFTEN COMINED WITH REGULAR INSULIN  ONSET: 1-3 HOURS  PEAK 5 TO 8 HOURS  DURATION: UPTO 18 HOURS LONG-ACTING INSULIN  DETEMIR (LEVEMIR), GLARGINE (LANTUS)  ONCE OR TWICE DAILY DOSING DEPENDING ON DOSE  NO PEAK; DURATION 18-24 HOURS  DOESN’T HELP WITH MEALS FIXED-COMBINATION INSULINS  EACH CONTAINS TWO DIFFERENT INSULINS IN FIXED AMOUNTS  ONE INTERMEDIATE-ACTING  EITHER ONE RAPID-ACTING (HUMALOG OR NOVOLOG) OR ONE SHORT ACTING TYPE (HUMULIN)  MANY DIFFERENT TYPES:  HUMULIN 30/70  NOVOLIN 30/70, 40/60, 50/50 (3 TYPES)  NOVOMIX 30  HUMALONG MIX 25 OR MIX50 SLIDING SCALE INSULIN DOSING  SC RAPID-ACTING OR SHORT-ACTING INUSLINS ARE ADJUSTED ACCORDING TO BLOOD GLUCOSE LEVELS  TYPICALLY USED IN HOSPITALIZED PATIENTS OR THOSE ON TPN/ENTERAL TUBE FEEDINGS  DISADVANTAGE: DELAYS INSULIN ADMINISTRATION UNTIL HYPERGLYCEMIA OCCURS, RESULTING IN LARGER SWINGS IN BLOOD GLUCOSE CONTROL  RECENT RESEARCH DOES NOT SUPPORT SLIDING SCALES, BUT THEY ARE STILL COMMONLY USED BASAL-BOLUS INSULIN DOSING  PREFERRED METHOD OF TREATMENT OF HOSPITALIZED PATIENTS WITH DIABETES  MIMICS HEALTHY PANCREAS  BASAL INSULIN IS A REGULAR/SLOW-ACTING INSULIN ORAL ANTIDIABETIC AGENTS  SIX CLASSIFICATIONS:  BIGUANIDES (METFORMIN)- TYPICALLY FIRST CHOICE  SULFONYLUREAS  AMINO ACID DERIVATIVES  MEGLITINIDES  THIAZOLIDINEDIONES  ALPHA-GLUCOSIDASE

BIGUANIDE  PROTOTYPE: METFORMIN (GLUCOPHAGE)  FIRST-LINE DRUG AND MOST COMMONLY USED SULFONYLUREAS  PROTOTYPE: GLYCLAZIDE (DIAMICRON)  MECHANISM OF ACTION: STIMULATES THE BETA CALLS OF THE PANCREAS MEGLITINIDES  PROTOTYPE: REPAGLINIDE (GLUCONORM) not as common  MECHANISM OF ACTION: SIMILAR TO SULFONYLUREAS BUT STRUCTURALLY DIFFERENT  USED IF PT HAS A SULFA ALLERGY OR TOLERANCE TO DIAMICRON THIAZOLIDINEDIONES (GLITAZONES)  PROTOTYPE: ROSIGLITAZONE (AVANDIA)  REFFERED TO AS INSULIN-SENSITIZING DRUGS  INDICATIONS: CAN BE USED IN PREDIABETICS TO REDUCE PROGRESSION TO TYPE 2 DM BY 60%; TYPE 2 DIABETES ALPHA-GLUCOSIDASE INHIBITORS  PROTOTYPE: ACARBOSE (GLUCOBAY)  LESS COMMONLY USED  MECHANISM OF ACTION: REVERSIBLY INHIBIT ALPHA-GLUCOSIDASE (ENZYME INVOVLED IN GLUCOSE UPTAKE) TO DELAY GLUCOSE ABSORPTION SODIUM GLUCOSE COTRANSPORTER 2 INHIBITORS  PROTOTYPE: CANAGLIFOZIN (INVOKANA)  NEW CLASS OF ORAL MEDICATION (2014) FOR TYPE 2 DIABETES GLUCOSE-ELEVATING DRUGS  USED TO TREAT SIGNIFICANT HYPOGLYCEMIA  DEXTROSE:  PARENTERAL ACCESS: 50% DEXTROSE (D50W) IF UNABLE TO TAKE ORALLY  GLUCAGON: IM TREATMENT Thyroid Replacement Medications Prototypes:  Levothyroxine (Synthroid)  Synthetic thyroid hormone (T4)  Desiccated thyroid (Thyroid)  Natural thyroid hormone (T3 and T4) Antithyroid Medications  Prototypes:  thiamazole (Tapazole) and propylthiouracil (PTU)  Mechanism of action:  Prevents thyroid gland from over-producing thyroid hormone  Inhibits iodine binding in the production of T3 and T4 precursors  May take several weeks/months before full effect Radioactive Iodine Therapy  Iodine I131:

 an isotope of iodine that emits radiation  Nuclear medicine treatment for overactive thyroid OR used to treat thyroid cancer  Taken orally; absorbed and concentrated by the thyroid gland  Works by ablation- destroys thyroid gland cells  One dose only Drugs to treat angina  Nitrates and nitrites  Beta-blockers  Calcium channel blockers Nitrates  Available in many forms:  SL, chewable tablets, oral capsules/tablets, IV, transdermal patches, ointments, spray  Large first-pass effect with oral forms  Prototype: Nitroglycerin  Contraindications:  Allergy  Severe anemia  Closed-angle glaucoma  Hypotension  Severe head injury  Use of erectile dysfunction drugs (Viagara, Cialis etc) Beta-Blockers  Mainstay in treatment of several cardiovascular diseases  Angina  Myocardial infarction  Hypertension  Dysrhythmias  Prototype: metoprolol (Lopressor) 

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Mechanism of action:  Block Beta-receptors on the heart:  Decrease heart rate therefore decrease myocardial oxygen demand and increased oxygen delivery to the heart  Decrease myocardial contractility, helping to conserve energy/decrease demand  Block harmful effects of catecholamines to improve survival after an MI Contraindications:  Systolic heart failure  Serious conduction disturbances  Caution: bronchial asthma  Diabetes: can mask hypoglycemia-induced tachycardia  Peripheral vascular disease: may further compromise cerebral or peripheral blood flow

Metoprolol  Cardio-selective beta-blocker  Used for treatment of angina but also used following MI and to treat hypertension  Reduces mortality rate in MI patients  Forms: oral (intermediate release and long acting) and parenteral forms  IV given to patients after MI Calcium channel blockers  Prototype: diltiazem (Cardizem)  Very effect for treating angina and hypertension 

Mechanism of action:  Cause coronary artery vasodilation  Cause peripheral arterial vasodilation  Reduces the workload of the heart  Depresses the automaticity of and conduction through the SA and AV nodes  Result: decreased myoca...