PHARR100 Midterm Review PDF

Mod 1 learning outcomes: 1. Discuss the influence of drug use by ancient civilizations on modern pharmacology What is the definition of a drug? Can you think of any drugs used by ancient civilizations that are still used today? Drugs acting against infectious disease (e.g. sulfa drugs, peni...

Mod 1 learning outcomes: 1. Discuss the influence of drug use by ancient civilizations on modern pharmacology What is the definition of a drug? Can you think of any drugs used by ancient civilizations that are still used today? Drugs acting against infectious disease (e.g. sulfa drugs, penicillin) Drugs acting on the brain (e.g. LSD) 2. Describe the process of developing a new drug and the conduct of clinical trials 3. Explain how drugs act on the body to produce their effect, and [explain why drug variability exists] - Genetic factors - Environmental factors - Disease states - Altered physiology - Presence of other drugs What do drugs normally bind to within the body to cause their effects? a)Acids b)Receptors c)Ligands d)Axons In your groups, using the white board, draw and explain: A dose response curve Efficacy Potency Therapeutic Range Explain agonist and antagonist in terms of the dose response curve A diagram of a graph Description automatically generated  4. Illustrate the path of a drug from when it enters to when it exits the body Routes of administration Order the routes of administration from fastest to slowest (oral, IV, sublingual) What is the most common route of administration? Absorption - Movement of the drug from site of administration into the blood - Must cross biological membranes - What is the definition of bioavailability? Distribution - Movement of the drug from the blood to the site of action - Depends on blood flow to the organ A diagram of a drug Description automatically generated 5. Explain how and why adverse drug reactions and drug-drug interactions occur Adverse effects of drugs - Extension of therapeutic effect - Allergic reactions - Teratogenesis - Withdrawal and addiction Therapeutic Index - TD50/ED50 - Higher the therapeutic index, the safer the drug Example: Drug A: TD50 = 50mg; ED50 = 10mg; What is the TI? Drug B: TD50 = 100mg; ED50 = 10mg; What is the TI? Which drug is safer? Drug-drug interactions - Absorption, metabolism, excretion Drug-food interactions - e.g. tyramine, grapefruit 6. Describe how nerve impulses travel throughout the body 7. Explain how drugs modify or restore the normal function of the nervous system - Glutamate - GABA - Dopamine - Norepinephrine - Acetylcholine - Serotonin Module 2 LO 1. Explain substance use disorder and describe the factors that influence this disease. What are the five criteria for substance use disorder (SUD)? - Social impairments - Risky use - Impaired control - Withdrawal - Tolerance LO1: Explain substance use disorder and describe the factors that influence this disease. Q. What happens to the dose response curve of a drug after tolerance has developed? T or F?: The withdrawal symptoms of a drug are often very similar to the primary therapeutic effects of the drug. Q. The primary hypothesis for the cause of addiction involves which neurotransmitter in the brain? 2. Discuss the properties of a substance that increase the potential for misuse and substance use disorder What are the five factors that contribute to the potential for misuse of a drug? - Nature of the drug - Route of administration - Amount/Frequency of use - Availability - Inherent harmfulness 3. Summarize the mechanism of action, main effects and toxicities, potential for misuse and substance use disorder, and therapeutic uses of common stimulant drugs. **Amphetamines** Main effects: - CNS excitation - Feeling of euphoria and reward - Appetite suppression - Increase in aggressive behaviour and mood swings Adverse effects: short and long term Therapeutic Uses: Narcolepsy, ADHD Potential for Misuse and SUD: Extremely high **Cocaine** Main effects: - CNS excitation - Feeling of euphoria and reward Adverse effects: long term Therapeutic Uses: Local anesthetic mouth/throat Potential for Misuse and SUD: Extremely high **Caffeine** Main effects: - Reduced fatigue, peripheral blood flow, mild stimulation of resp rate - High doses: irritability, nervousness, psychomotor agitation - Specific circumstances: smoking; pregnancy SUD: Misuse potential is low Tolerance, mild withdrawal, mild addiction Therapeutic Uses: Stimulate breathing in preterm newborns **Nicotine** Main effects: - Mild euphoria, concentration - Long-term adverse effects: cardiovascular disease, lung disease, and cancer due to smoking SUD: Misuse potential is very high Withdrawal, highly addictive Therapeutic Uses: Smoking cessation 4. Discuss the use of drugs in sports and explain why many drugs are banned by all sports authorities Amphetamines Anabolic steroids Benzodiazepines Blood doping and erythropoietin Diuretics Mod 3 LO 1. Compare and contrast the classes of sedative-hypnotics in terms of beneficial and adverse effects and therapeutic uses. Q: Describe the mechanism of action of the barbiturates and benzodiazepines. WHAT ARE THE ADVANTAGES OF BENZODIAZEPINES OVER BARBITURATES? - Benzos have a wide spectrum of use. - More selective in action than barbs, barbs depress glutamatergic systems. - Benzos high therapeutic index. - Low effect on REM sleep. - Less respiratory depression. - Low misuse liability. - Less severe withdrawal with benzodiazepines. 2. Describe the effect of short-term and long-term use of alcohol and cannabis on human health. **Cannabis:** CNS depressant, euphoriant, hallucinogen (hallucinogen at high doses) CB1 receptors in CNS; CB2 receptors in periphery (e.g. lymphocytes) Anandamide = endogenous ligand for CB receptors Cannabis has actions both within the CNS and elsewhere Impairment; automobile driving SUD: tolerance, withdrawal, and addiction **Alcohol:** CNS depressant Metabolism -- what is different from majority of other drugs? Low and high dose effects Alcohol use during pregnancy Misuse potential: moderate SUD: tolerance, withdrawal, and addiction 3. Summarize the social and legal issues associated with the use of CNS depressant drugs. Opioid crisis: Harm reduction: Decrease stigmatization: 4. Explain the mechanism of action and adverse effects of opioid analgesics. Endogenous Opioids - Dynorphins, enkephalins, endorphins Receptors - Mu, delta, kappa MOA - Reduce neurotransmitter release - Reduce emotional reaction Adverse Effects - Sedation - Respiratory depression - Miosis - Constipation Opioid Use Disorder - Tolerance, withdrawal, addiction - Tolerance is selective - GI effects Example MCQ 1\. The TD50 of a drug in rats was found to be 50 milligrams/kilogram. The ED50 of the same drug in rats was 1 milligram/kilogram. From this information, one can calculate that the therapeutic index of the drug in rats is: a\) 0.02 b\) 50 c\) 49 d\) 51 2. Which one of the following statements regarding drug administration is correct? a\) With oral administration of a drug, there is always an excellent relationship between the dose of a drug administered and its concentration in the blood. b\) After injection of drugs into skeletal muscle, the drugs are generally slowly absorbed into the blood supply of the muscle and will usually act after a period of 20 hours. c\) Virtually no poisonous materials are readily absorbed through the skin as the skin is an effective barrier. d\) If specially purified water is not used for dissolving drugs prior to intravenous injection, the pyrogens present in the water could cause fever. 3\. A drug is administered orally at the same time as an antacid preparation. The two drugs combine together in the intestine to form a complex that cannot cross into the blood. This reaction is best described as? a\) A drug-drug interaction affecting absorption. b\) A drug-food interaction affecting metabolism. c\) A drug-drug interaction affecting excretion. d\) A drug-food interaction affecting absorption. 4\. The major inhibitory neurotransmitter in the CNS is: a\) Norepinephrine b\) Gama-aminobutyric acid (GABA) c\) Acetylcholine d\) Curare 5\. Which one of the following statements regarding alcohol is correct? a\) It is slowly absorbed from the stomach and small intestine b\) It readily gains access to the brain, but not the placenta c\) The amount of alcohol metabolized per hour increases the more you drink d\) It binds to the chloride channel at a different spot than benzodiazepines 6\. Which one of the following statements regarding SUD is correct? a\) Drug tolerance is defined as a state in which repeated administration of a given dose of the drug has progressively greater pharmacological effect. b\) Addiction is characterized by the appearance of a withdrawal syndrome when the drug is stopped abruptly. c\) Drug use is reinforced by the pleasurable effects and is mediated by dopaminergic neurons. d\) Drug withdrawal rarely occurs under conditions when the drug is prescribed by a physician. 7\. Drug A can only relieve pain of mild intensity. Drug B, on the other hand, relieves pain of very marked intensity. From this information, one can conclude that: a\) Drug A has greater efficacy than Drug B. b\) Drug B has greater efficacy than Drug A. c\) Drug A is more potent than Drug B. d)Drug B is more potent than Drug A. 8\. Which one of the following CNS stimulants may be used clinically to treat narcolepsy a)Caffeine b)Nicotine c)Amphetamines d)Cocaine 9\. Which one of the following statements correctly applies to the performance enhancing properties of the anabolic steroids? a\) They are more effective in males than in females. b\) They are usually associated with an increase in fertility. c\) They will very minimally increase lean body mass in users that follow an exercise regime. d\) They are associated with several toxicities 10\. A common adverse effect of opioids is: a)Dilation of pupils b)Diarrhea c)Respiratory depression d)High body temperature