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219 Cards in this Set
- Front
- Back
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Opium |
Derived from Opium Poppy plant - Contains Codeine and Morphine |
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Codeine |
- Pain relief of moderate pain - constituent of Tylenol 1 - 0.5% |
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Morphine |
- 10% - named after Morpheus- god of dreams - relieve intense pain |
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Ma Huang |
- originated in ancient china - ephedrine - asthma relief - derivative of decongestant |
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Ancient Egypt |
Ebers Papyrus - medical textbook - found relevant info on purgatives - Senna discovered |
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Curare |
Amazonians dipped arrows to paralyze - used for anaesthetics |
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Ergot |
poisonous fungus grows on top of rye - ground together with rye in Middle Ages, epidemic due to bread - 20 000 people killed during Russian epidemic |
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Ergot effects |
- hallucinations - constriction of blood vessels - violent uterus contractions |
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Ergotamine |
used to treat migraines by constricting arterial vessels - |
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Ergonovine |
Previously used to hasten birth, no longer used since effects have proven to deliver too quickly and risk injury of mother and child |
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Reserpine |
Derived from Rauwolfia plant - used to lessen anxiety - lessen fierceness in dogs |
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Chlorpromazine |
- obtained by synthetic procedures - used on anxious, tense, hostile patients |
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Lysergic Acid Diethylamide |
- Albert Hofmann synthesized LSD 1943 - LSD similar chemical structure to ergotamine and ergonovine - mental illnesses occur when brain releases potent substances that produce psychic disturbance |
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Nitrous Oxide |
-laughing gas - helpful anaesthetic agent |
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Ether |
- similar properties to nitrous oxide |
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1900's Organoarsenicals |
Paul Ehrlich - arsenic and organic molecules which bind to parasites - found cure for syphillis - "father of chemotherapy" |
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1930's Sulfa |
-antibacterial compounds - first successful synthetic drugs for the treatment of bacterial disease |
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1940's Penicillin |
Alexander Fleming - first antibiotic WW2 - therapy of gram positive bacterial disease |
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1950 Streptomycin |
Selman Waksman - different antibiotic - treatment of tuberculosis and gram negative bacterial diseases |
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Drug Discovery |
Identifying potential biological target , finding compound that will bind well |
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Preclinical Studies |
- conducted prior to testing new drug - molecular and cellular studies |
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Toxicology Studies |
- determines effects on organs other than target - adverse drug effects - all drugs have toxicity - expensive studies - may take up to 6 years |
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Pharmacology Studies |
- detailed mechanism of action of drug - ex. HOW does drug lower blood pressure? |
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Initial Clinical Trial Steps |
1. Submit proof of safety and efficacy in animals to gov. regulatory agency 2. Methodology of proposed trial on humans 3. submission evaluated by agency- if passed, investigation can begin - 5-30 compounds make it through preclinical testing |
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Phase 1 |
- 20-50 young healthy people - careful evaluation of absorption, distribution, elimination and adverse effects |
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Absorption Process |
diffusion through lipid bilayers containing proteins - levels of high to levels of low concentration l - IMPORTANT lipid solubility carry molecules across membrane to bind and carry down then release |
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Distribution |
Movement of drug from blood to site of action and other tissues - rate at which drugs distribute depends on blood flow |
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CNS (The Brain) |
- processes and receives information - Initiates a response - stores memory - generates thought and emotion |
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CNS (Spinal Cord) |
controls motor outflow to muscles controls sensory input controls reflex activity
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Forebrain |
- cerebral cortex - thalamus - limbic system - hypothalamus - pituitary gland |
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Midbrain |
relay centre for eye and ear signals and stimuli - connects forebrain and hindbrain |
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Hindbrain |
- pons - medulla - cerebellum |
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Cerebral cortex (cerebrum) (FB) |
- rich in nerve cells - sensory and motor coordination - mental processes - intelligence, memory - judgement thought, speech, emotion - stimulated or depressed by drugs |
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Thalamus (FB) |
Relay centre - coordinate filter incoming signals - appreciation of painful sensations |
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Limbic System (FB) |
- integrates memory, emotion, reward - Dopaminergic reward centres (targets for drug of abuse) |
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Hypothalamus (FB) |
- controls involuntary functions necessary for living - feeding, drinking, sexual and emotional responses - number of drugs can affect |
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Pituitary Gland (FB) |
- secrets hormones - control of growth, metabolism, behaviour |
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Pons (HB) |
- connects midbrain to medulla and cerebellum - conducts signals from cerebral cortex down to medulla and cerebellum |
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Medulla (HB) |
- site of origin of many cranial nerves - regulation of respirartion, heart rate, blood pressure - number of drugs depress respiration and blood pressure by depressing medulla |
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Cerebellum (HB) |
- coordination and posture - does NOT initiate movement - organizer of voluntary activity - drugs that affect it will cause ataxia |
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Ataxia |
loss of coordination ex. caused by alcohol |
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Neuron |
- functional unit of brain - nerve cell capable of generating and transmitting electrical signals - brain contains 90 billion - 2 types of projections: dendrites and axons |
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Neurogenesis |
The continuous generation of new neurons |
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Neuroplasticity |
The constant reshaping of the connection of neurons |
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Dendrites |
- short, highly complex branch looking things - receive incoming info through receptors -electric current generated, directed down the neuron |
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Cell Body (soma) |
- contains nucleus and surrounding cytoplasm - cytoplasm's abundant vesicles that can be secreted |
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Axon |
- Single fibre that from cell body to synapse - carries info away from cell body and dendrites by electrical impulses |
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Synapse |
- Junction between 2 neutrons - area where one neurons axon ends and another neurons dendrite or cell body begins |
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Synaptic Transmission |
Passage of a signal from one neuron to another - very rapid - usually chemical in nature (substance released to activate next neuron) |
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Neurotransmitters |
Endogenous chemicals that transmit a signal between 2 neurons |
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Glutamate |
- primary excitatory neurotransmitter in CNS - acts on glutamatergic receptors - important for learning |
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Gamma- Amino Butyric Acid |
- Primary inhibitory neurotransmitter in CNS - high concentration in cerebral cortex, hippocampus, cerebellum - Some CNS depressants enhance GABA receptor function |
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Acetylcholine |
- produces excitatory response in CNS - Receptors that bind acetylcholine are called Cholinergic receptors |
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Cholinergic receptors |
Nicotinic and Muscarinic Receptors |
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Nicotinic Receptors |
- stimulated by nicotine - found in certain brain regions |
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Muscarinic Receptors |
- Stimulated by muscarine - found in many brain regions - learning, memory, cognitive function - drugs that block action at these receptors cause amnesia. - Associated with Alzheimers |
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Catecholamines |
Dopamine and Norepinephrine |
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Dopamine |
- some hormonal systems - motor coordination, motivation and reward - associated with Parkinson's and schizophrenia |
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Norepinephrine |
- Alpha and Beta - usually leads to excitation of cell - CNS stimulants |
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Serotonin |
- involved in anxiety and hypo-activity implacated in depression - some CNS stimulants act by increasing serotonin at synapse |
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Endogenous Opioid Peptides |
- Enkephalins - Endorphins - Dynorphins - Mu, Delta, Kappa |
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Factors Influencing substance abuse |
1. Genetic factors 2. coexisting disorders 3. environmental factors 4. developmental factors |
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The dopamine Hypothesis |
1. drugs of abuse increase dopamine in reward systems of brain 2. also responsible for natural reward (food and sex) and stimulus related rewards ( video games, gambling) |
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Characteristics of addictive drugs |
1. increase dopamine 2. produce novelty 3. reduce anxiety |
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Increasing dopamine |
CNS Stimulants - cocaine - amphetamines - nicotine Opioids - Morphine - heroin -oxycontin - alcohol -cannabis |
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Produce Novelty |
- LSD - Ecstasy (MDMA) |
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Reduce anxiety |
- Benzodiazepines - Barbiturates |
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Drug abuse potential factors |
1. dependance liability 2. liability 3. inherent harmfulness |
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Dependance liability |
tendency of drug causing dependance and addiction 1. nature of drug 2. route of administration 3. amount/frequency of use |
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Substance dependance |
complex disease process of CNS the requires repeated consumption or chronic use of substance 1. drug dependance and withdrawal 2. drug tolerance 3. drug addiction |
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Opiates |
Morphine Codeine Heroin |
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CNS Depressants |
Ethanol Sedatives Hypnotics |
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CNS Stimulants |
Amphetamines Cocaine |
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Amphetamines |
- synthetic organic compounds - Methamphetamine - Dextroamphetamine Related compounds: - MDMA - Ritalin (ADHD) |
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CNS effects of amphetamines |
1. decreased sensory threshold for transmitting input to cerebral cortex, leading to excitation 2. feeling of reward and euphoria 3. increase in aggressive behaviour and mood swings 4. appetite suppression |
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Cocaine in CNS |
1. inhibits active reuptake of dopamine and serotonin into presynaptic nerve terminal 2. increases activation of postsynaptic receptors |
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Absorption of Nicotine |
A: Inhalation, absorbed through gastrointestinal trust, oral mucosa - depth of inhalation and frequency of smoking |
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Distribution of Nicotine |
throughout body, rapid gains to brain |
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Metabolism of NIcotine |
Metabolized in liver |
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Excretion of Nicotine |
Excreted in urine, half-life is about 2 hours |
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Caffeine |
- blood levels significant after 30 mins - half life = 2.5-10 hours - metabolism slowed by pregnant women - metabolism increased by nicotine - low abuse liability |
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Overall Amphetamines |
- blocks VMAT, increases dopamine and norepinephrine at synapse. Short term: euphoria, overstimulation, insomnia, appetite suppression Long term: psychoses, elevated blood pressure, appetite Abuse: Extremely high Tolerance, Dependance, Addiction: YES uses: narcolepsy, ADHD |
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Overall Cocaine |
-Blocks reuptake of dopamine, increases dopamine at synapse Short term: same as Amphetamines but shorter Long term: same as Amphetamines but also impaired sexual function Abuse potential: extremely high Tolerance, Dependance, Addiction: YES uses: rare anaesthetic |
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Overall Nicotine |
- Stimulates nicotinic receptors Short Term: enhanced arousal, more concentration, relaxation, slight euphoric feeling Long term:cardiovascular and lung disease, cancer Abuse: very high Tolerance:No Dependance: yes Addiction: yes |
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Overall Caffeine |
- Prevents inhibition at adenosine receptors Short term: decreases fatigue, increase mental performance motor activity Long term: Restless, nervous, insomnia abuse: low Tolerance: in some people Dependance and addiction: yes |
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Amphetamines in Sports |
Endurance- duration of performance extended by 40% after 10 mg of methamphetamine Speed- when given 10 mg, 14/15 swimmers were faster and 73% improved times |
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Anabolic Steroids |
- reduces androgenic effects (effects on secondary male sex characteristics) - increase anabolic (increase of muscle mass) effects |
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Anti-catabolic effects |
blocks proteins from muscles being used for training |
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Anabolic effects |
- protein production and supplementation = critical to athletes -Roid rage- cause aggression in athletes |
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Females and Anabolic steroids |
- increased facial and body hair - lowered voice - enlarged clitoris - coarser skin, acne - aggression |
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Anabolic Steroids Toxicities |
1. mood swings 2. severe acne 3. cardiovascular disease 4. altered liver function 5. reduced testosterone levels |
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Diuretics |
enhance excretion of salt and water through kidneys - allows athlete to compete at lower weight class |
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Blood Doping and Erythropoitin |
BD: taking blood cells out and rein fusing them to give more oxygen EPO: injection used to boost red blood cells, stimulates bone marrow Hematocrit levels: volume percent of red blood cells in blood |
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CNS Excitation |
1. excitatory neutrons release glutamate (neurotransmitters) - neurons fire when exhibitory exceeds inhibitory 2. inhibitory signals from GABA neurons increase with most sedative hypnotics 3. Increase in GABA firing = decrease in glutamate firing |
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Drugs that bind to Chloride channel |
- Benzodiazepines - Flumazenil - Zolpidem - Barbiturates |
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Benzodiazepines |
- usually capsule or tablet - increases frequency of opening of chloride channel - among drugs most common for overdose - used to treat alcoholism |
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benzodiazepines 2 |
- very high therapeutic index - decrease aggression - skeletal muscle relaxation - anti-anxiety, sedation, amnesia - produce REM sleep -anticonvulsant action - antidote exists (flumazenil) |
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Benzodiazepines short term CNS effects |
- relaxation, calmness, relief from anxiety and tension - drowsiness, lethargy, fatigue, impairment from memory |
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Benzodiazepines short term lung effects |
respiratory depression only after rapid intravenous administration |
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Benzodiazepines short tern MC effects |
patients should refrain form driving, operating heavy machinery - responses exaggerated as dose increases |
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Benzodiazepines long term effects |
- some will demonstrate no intoxication - others will show chronic sedative-hypnotic effects- disorientation, slurred speech, impaired judgement |
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Benzodiazepines effects special pop. |
Pregnant: crosses placenta, distributes into fetus - leads to death for fetal abnormalities Elderly: can produce cognitive dysfunction - metabolized much slower, leads to over-sedation- falls and injury |
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Abuse of Benzodiazepines |
- low abuse liability - low inherent harmfulness - can develop but not likely - low dependence risk - addiction may develop |
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Flumazenil |
Receptor antagonist that undoes effects of benzodiazepines |
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Zolpidem and Z drugs |
- bind to subset of GABA receptors- cause sedation - disturb sleep patterns less - more sedative effects - use with caution in elderly |
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Barbiturates (Anti-epileptic) |
- increases time of opening of chloride channel - for epilepsy: oral admin - for anaesthesia: intravenous |
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Classification of Barbiturates |
1. Long acting - 1-2 days - phenobarbital 2. Short-acting- 3-4 hours- secobarbital 3. ultrashort acting- 20 mins- thiopental |
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Barbiturates clinical use |
ultrashort and short agents: anaesthetic uses longterm: anti epileptics |
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Barbiturates lethality |
- Lethality common - No antidote - death can be from withdrawal |
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Barbiturates Pharmacology |
- low therapeutic index - full spectrum of CNS depression - suppress REM sleep - depress respiratory system - high doses depress cardiovascular system |
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Barbiturate Short term effects |
- euphoria, tranquility, relaxation, mild euphoria, reduced interest in surroundings -dizziness and mild motor coordination impairment - may induce sleep - pleasurable intoxication |
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Barbiturate long tern effects |
- chronic inebriation- mood swings, depression, hostility |
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Barbiturate Abuse |
- higher abuse liability than alcohol - sometimes injected for a rush - very high inherent harmfulness because respiratory depression - very addictive- can come from regular use |
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Barbiturate tolerance |
1. very rapidly- sleep induction and mood effects 2. more slow- motor coordination, reaction time 3. very slowly- Anticonvulsant actions |
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Barbiturate dependance |
- tremors, anxiety, weakness, insomnia, postural hypotension - progress to seizures, delirium, visual hallucinations, high body temp |
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GHB (gamma-hydroxybutyic acid) |
- antagonist of subset of GABA - sedation and anaesthesia - high dependance liability - not used in north america - date rape drug |
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Buspirone |
- acts at serotonin receptor - used for GAD - no additive effect with other sedative-hypnotics |
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Ethanol absorption |
- rapid absorption from stomach and small intestine - Absorption rate affected by: 1. stomach-emptying time 2. ethanol concentration in gastrointestinal tract - max BAC after having last drink = 30-90 mins |
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Ethanol distribution |
- throughout total body water, gains access to brain - goes through placenta to fetus |
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Ethanol Metabolism |
1. ethanol to acetaldehyde by ADH enzyme 2. Genetic variants in gene that codes for ADH exist 3. Acetaldehyde converted to acetic acid by ALDH 4. acetate further metabolized by number of tissues |
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Ethanol excretion |
95% excretion by biotransformation in liver - mainly urine - 5% in breath |
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Ethanol CNS effects |
- general CNS depressant ( bac level) |
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Ethanol short term effects |
- flushing of vessels to skin (vasodilation) - increased gastric secretion - depression of cardiovascular system - irritate stomach lining- vomiting and ab pain - inhibit glucose production - lower blood sugar levels |
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Ethanol short term high dose adverse effects |
- blackouts - mental health - drinking and driving - violence - coma and death |
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Ethanol long term effects |
- alcohol dementia- less neural connections in brain - alcoholic cardiomyopathy (destruction of heart muscle) - increase hypertension and stroke Liver: 1- fatty liver: asymptomatic and reversible 2. Alcoholic hepatitis:abstinence will reverse, some severe conditions 3. Cirrhosis:non reversible- severe damage |
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Fetal Alcohol Syndrome (FAS) |
- impairment in attention, learning, memory - pre and post natal birth deficiency - face abnormalities: low nasal bride, short nose, small facial features |
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Ethanol Abuse |
- significant reinforcing properties - moderate dependance liability - tolerance to chronic use occurs - |
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disulfuram |
-inhibits hepatic aldehyde dehydrogenase - increases acetaldehyde = cardiovascular effects aversive |
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Naltrexone |
-opioid antagonist - diminishes alcohol cravings - assists abstinence maintenance - blocks dopaminergic reward pathways |
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Acomprosate |
- Weak Glutamate receptor antagonist - GABA activator - no great effects proven |
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Ethanol MOA |
Binds to chloride ion channel, augments GABA signalling |
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Alcohol |
Can be used as antidote for methanol poisoning |
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Cannabis |
Euphoriant, CNS depressant, hallucinogen at high doses - Hashish= dry resin from compacted flowers |
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Cannabis MOA |
Anandemide goes from post-synaptic neutron to CB1 receptors on the presynaptic neutron, inhibiting release of excitation of neurotransmitter glutamate |
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CB1 receptors |
- found all over brain - mediate colour, sound, taste - hippocampus- learning of memory |
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CB2 receptors |
- found outside CNS - involved in inflammation |
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Inhalation of THC |
- rapid onset immediate action - effect lasts 3-4 |
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Ingestation of THC |
- slow and incomplete absorption - onset of action delayed 30-60 minutes - less effect |
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THC CNS effects |
- relaxation and drowsiness - feeling of well being and euphoria - impaired motor coordination |
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THC cardiovascular effects |
- increased heart rate - increased blood flow to extremities - postural hypotension |
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THC GI tract effects |
- increased appetite - dryness of mouth and throat |
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THC other effects |
- reduction of sex drive in males - disruption of ovarian cycle - hangover |
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THC long term use |
- loss of short term memory - lack of concentration - motivational syndrome permanent effects unknown - irreversible increased heart rate |
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THC Smoking effects |
- bronchitis - asthma - sore throat - chronic irritation to respiratory tract - lung disease/cancer |
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THC fertility effects |
- decreased sperm count - cognitive deficits - impulsiveness - hyperactivity |
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Medical uses |
- increases appetite (for sick people) - treats neuropathic pain - epilepsy, glaucoma, migraines |
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THC abuse |
- dependance liability is low -moderate - tolerance occurs - dependance occurs at high dose use - addiction more risk for users for psychological stress |
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Narcotic Analgesics |
any drug derived from opium ex. morphine, codeine |
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Opioid |
natural/synthetic substance which exerts actions of body similar of those induced by morphine and antagonized by naloxone |
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Opioid receptors: MU |
- moderate analgesic - responsible for morphine- mediated depression of respiration in brain stem |
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Opioid receptors: Kappa |
-involved in analgesia, miosis,(pin-point pupil), dysphoria (dissatisfaction, unease) |
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Opioid receptors: delta |
- involved in analgesia at spinal cord & brain - modulate emotional response to opioids |
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Opioid MOA |
reduce release of transmitters in charge of pain impulses (activating inhibitory pathways to block pain input) reduce emotional pain reaction |
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Morphine Short term effects |
- taken in pill, smoked, sniffed or injected - usually taken alone -may be in combo with coke and methamphetamine |
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Heroin short term effects |
- more potent than morphine but not more efficacious - rapidly converted to morphine in body -injected, sniffed, smoked |
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Opioid Short term effects |
- analgesia - sedation and hypnosis - suppression of cough centre in medulla - respiratory depression - endocrine effects - mitosis - heart rate and thermoregulation - constipation |
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Opioid long term effects |
-mood instability - constipation - reduced libido - respiratory impairment - pupils constrict |
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Opioid therapeutic use |
- relief of severe pain - treatment of diarrhea - cough suppression |
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Opioid Dependance |
Withdrawal syndrome - sweating, restlessness, increased respiratory rate - cramping, vomiting |
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Causes of withdrawal syndrome |
- particular drug - chronicity and pattern of use - typical daily dose -place of administration - health of user |
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Methadone |
used to treat opioid dependance - synthetic opioid - long Half live risk reduction method - taken orally 1. cessation of drug use 2. methadone maintenance |
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Selective toxicity |
use of drugs to harm invading organism with harming host |
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Antifungal drugs |
- amphotericin B - fluconazole - itraconazole - voriconazole |
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Amphotericin B |
- severe fungal infections - binds to ergosterol - combo results in leakage across fungal membrane - intravenous administration - kidney toxicity |
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Imidazoles |
-inhibit P450 -- inhibit ergosterol synthesis - taken orally |
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P450's |
- enzyme that metabolizes many drugs |
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Virus |
small, infectious agent only able to multiply in living cells of other organisms |
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Viral cycle |
1. attachment 2. entry 3. replication 4. biosynthesis 5. assembly 6. release |
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Drugs for Influenza |
1. amantidine 2. tamiflu |
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Amantidine |
-inhibits coating of viral RNA within infected cells - prevents viral replication - viral resistance is problem |
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Tamiflu |
- neuraminidase inhibitor - prevent neighbouring cells from being infected |
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Acyclovir |
- inhibits viral DNA replication - activates acyclovir into active form - decreases frequency of reoccurrence of genital herpes - acyclovir is drug of choice for HSV |
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Varicella-Zoster Virus |
- virus that causes chicken pox and shingles |
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HSV |
Herpes Simple Virus |
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Antibiotic |
chemical substance that surpresses growth of bacteria and eventually may kill it - purpose is to stop bacterial infection |
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Bacteriostatic effects |
inhibits growth and reproduction of bacteria |
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Bactericidal effects |
directly kills bacteria |
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Cell Wall |
rigid outer layer - completely surrounds cytoplasmic membrane |
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Peptidoglycan |
- contained in cell wall - complex, cross linked polymer of polypeptides an polysaccharides |
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Cross links structural rigidity |
- maintain cell shape and integrity - prevents cell lysis from high osmotic pressure |
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Gram positive bacteria |
thick peptidoglycan layer, - no outer membrane |
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Gram negative bacteria |
thin peptidoglycan layer -outer membrane |
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Classification of antibiotics |
1. spectrum of affected microorganism 2. based on biochemical pathway targeted In microorganism |
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Narrow spectrum antibiotics |
only useful against particular species of microorganisms - Penicillin G only effective against gram positive bacteria |
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Broad spectrum antibiotics |
effective on wide range of organisms effective on gram positive and negative - Tetracyclines |
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Penicillin MOA |
- interferes with new bacterial cell wall formation - results in cells forming with no cell wall - selectively toxic to bacteria |
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Protoplasts |
- fragile - can readily burst - cells with no cell wall |
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Adverse Penicillin effects |
mainly allergic reactions - rash - fever - itchy hives - diarrhea - face and tongue swelling rare cases: - respiratory issues, fall in blood pressure |
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Penicillin G- Natural |
- narrow spectrum antibiotic - targets mainly gram positive bacteria - pneumonia, middle ear infections, meningitis, syphilis |
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Penicillin V- semisynthetic |
- more stable than G, less absorbed by stomach acid - achieves higher blood pressure levels of antibiotic - V is prescribed for oral admin instead of G |
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Methicillin |
- resistant to attack by penicillinase |
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Penicillinase |
enzyme that breaks down penicillin - production creates resistance to penicillin G |
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Ampicillin and Amoxicillin |
broader spectrum of antibacterial activity than penicillin G - useful against range of gram negative bacteria infections - ex. urinary tract infections |
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Augmentin |
combinations of semisynthetic penicillins + inhibitor of penicillinase - combat penicillinase producing strain of bacteria |
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Cephalosporins |
similar compound to penicillin but more resistant to penicillinase -selective inhibitors of bacterial cell wall synthesis - divided into 4 generations depending on spectrum of activity |
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Cephalosporins Adverse effects |
- fever and skin rashes - renal toxicity |
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Fluoroquinolones |
class of synthetic micro bacterial agents - ex. ciprofloxacin - IV or oral admin - gram pos or neg bacteria - inhibit bacterial DNA synthesis |
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Inhibitors of protein synthesis- Tetracyclines |
- first broad spectrum antibiotic activity - exerts bacteriostatic effects by bacterial protein synthesis |
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Tetracycline MOA |
- bind to 30S subunit of mRNA- ribosome complex - prevents amino acids in protein chain, inhibits protein synthesis |
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Tetracycline Adverse Effects |
- nausea, vomiting - diminished bone growth - teeth discolouration - - strong avidity for calcium- no pregnant women or children under 12 -can deteriorate into toxic degradation production |
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Macrolides |
- gram positive bacterial infections - given when patients allergic to penicillin |
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Macrolide MOA |
bind to 50s ribosomal subunit on tRNA and block peptide block formation |
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Macrolide adverse effects |
- nausea - vomiting - diarrhea |
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Food and Drug Act |
controls safety, efficacy, advertising and sale of products |
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Grandparenting |
process where regulations do not apply to those already on the market |
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using OTC guidelines |
1. illness and symptoms are mild 2. should be familiar with symptoms 3. self-medication should not exceed 2 weeks |
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selection of appropriate OTC |
- proven efficacy - have simplest formulation - list all ingredients - come in appropriate dosage form - known level of toxicity |
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Types of OTC |
1. internal analgesics 2. antihistamines 3. drugs for excess stomach acid 4. decongestants 5. cough suppressants 6. expectorants 7. sleeping aids 8. laxatives 9. antidiarrheals 10. 0.5% hydrocortisone 11. sunscreens |
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internal analgesics therapeutic uses |
1. effectively relieves pain, fever, and inflammation 2. low doses have been shown to prevent stroke and heart attack |
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internal analgesics mechanism of action |
1. pain, fever, and inflammation: ASA inhibits synthesis of prostaglandins, which are endogenous substances that enhance mediation of pain and fever and inflammation 2. stroke and heart attack: ASA inhibits platelet aggression and hence, clot formation |
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ASA adverse effects |
-tinnitus - reyes syndrome (affects CNS of children) - allergic reactions - gastric irritation |
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internal analgesics: acetaminophen |
1. effective analgesics and antipyretic, not effective anti-inflammatory 2. available in liquid preparation - good for kids |
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Acetaminophen MOA |
Inhibition of prostaglandin synthetases, which control the formation of prostaglandins |
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Acetaminophen Overdose |
Therapeutic dose = mild effects - can lead to fatal liver injury |
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NSAIDS MOA |
decrease production of prostaglandiins block cyclooxygenase (COX1 & cOX2) |
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Protective Prostaglandins |
- gastroprotection - platelet aggregation - renal protection - vasodilation - bronchodilation |
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Inflammatory Prostaglandins |
- inflammation - pain -fever - decreased platelet aggregation |
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NSAIDS adverse effects |
1. gastric irritation 2. skin rash 3. dizziness 4. fluid retention |
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Antihistamines |
block histamine receptors, inhibits binding of histamine to its receptors - 1st generation cause sedation and drowsiness - 2nd gen |
