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49 Cards in this Set
- Front
- Back
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Three examples of poisons and toxic substances |
calabar bean - used in Africa to identify sorcerers curare - used in amazon causes paralysis and death ergot - rye fungus (causes blood vessel constriction, abortion etc (like LSD)) |
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Digitalis purpurea has what effect |
performance of the heart muscle.Digoxin is also used to treat certain types of disordered rhythms of the heart, known as arrhythmias.
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Nitroglycerin has what effect |
treating angina pectoris (Latin for choking in the chest). Nitroglycerin dilates (opens up) blood vessels in the heart and elsewhere in the body. This action of nitroglycerin increases the supply of oxygen to the heart, and decreases the oxygen requirement of the heart, thus relieving pain. |
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Quinine has what effect |
Quinine is an important drug in the treatment of malaria. Drug improves heart arrhythmias
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reserpine and chlorpromazine have what effect |
converting the anxious, tense, and hostile person into someone who is placid and tranquil. |
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Anaesthetics have what effect |
similar to nitrous oxide. Reduces pain |
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Paul Ehrlich |
Father of chemotherapy, led to a dramatic cure for syphilis
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Gerhard Domagk |
Introduced sulfa drugs, first successful synthetic drugs for the treatment of bacterial disease
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Alexander Fleming |
Discovered the first antibiotic, penicillin |
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Selman Waksman |
Discovered streptomycin, turning point for treatment of tuberculosis and gramnegative bacterial diseases.
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Hallucinogens examples |
mescaline, LSD |
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Analgesics (pain relieving drugs) examples |
morphine, codeine, heroin, aspirin, acetaminophen |
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Cardiovascular drug examples |
digoxin, nitroglycerin, amyl nitrite, quinidine, reserpine |
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Antimicrobial drug examples |
organoarsenicals, sulfa, penicillin, streptomycin |
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Anaesthetics drug examples |
nitrous oxide, ether |
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Drugs used in psychiatry examples |
chlorpromazine, reserpine |
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Stages in Drug development |
A) Drug discovery 1. Research and discovery 2. Preclinical testing B) Clinical trials 3. Phase 1 4. Phase 2 5. Phase 3 6. Phase 4 |
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Purpose of Preclinical studies |
Determine the safety and tolerability of the new drug.
Determine the detailed mechanism of action of the new drug |
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Purpose of Clinical Trials |
Since differences between humans and animals exist, clinical trials are the only studies that will tell us if a drug is truly safe and effective in humans for the intended purposes. |
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Phase 1 of clinical |
The absorption, distribution, elimination and adverse effects of the new drug are carefully studied.Whether the drug is effective is not assessed in this phase.
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Phase 2 of clinical |
The objective of this phase is to determine whether the drug is effective in treating the condition for which it is recommended for, in a limited number of people.drug is given to patients with the disease for which the drug is designed to treat, and the effect is studied. Careful attention is paid to the safety of the drug. Phase 2 studies are often called ‘proof of concept’ studies.
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Phase 3 of clinical |
The safety and efficacy of the drug is carefully studied. Phase 3 trials are also called ‘controlled trials’ or ‘efficacy trials’. If the drug is found to be safe and effective in the Phase 3 trial, it will be released for marketing and general use.
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Phase 4 of clinical |
Surveillance of the effects of drugs are required after the drug is released for general use. This phase is therefore referred to as postmarketing surveillance. |
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Conducting randomized trials requires 10 factors: |
1. Target population 2. Inclusion and exclusion criteria 3. Ethical consideration and consent 4. Comparator 5. Randomization 6. Blinding 7. What is measured 8. Compliance 9. Quality of life 10. Analysis |
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Receptors |
are normally bound to and activated by endogenous ligands, which are substances ordinarily found in the body, such as hormones and neurotransmitters. Drugs modify the interaction between endogenous ligands and their receptors, and can either increase or decrease the activity of the receptors
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antagonists |
Drugs that bind to and stimulate a receptor are called agonists and drugs that bind to but block the response at a receptor |
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The dose response relationship |
the intensity of the pharmacological effects produced by a drug increases in proportion to the dose |
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Dose Response Curve |
A dose response curve is a graphical representation of how much drug you need in the body to see a specific effect. The effect of the drug is on the yaxis and is plotted on a linear scale, with the maximal response the body can produce set at 100%. The dose of the drug is on the xaxis of the graph and is plotted on a log scale. A generic dose response curve is shown adjacent. |
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ED50 |
the dose of drug that is effective in 50% of a population |
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Efficacy: |
The maximum pharmacological response that can be produced by a specific drug in that biological system. It is different from potency in that the amount of drug needed does not matter, what matters is the maximum effect that the drug can produce. Clinically, efficacy is more important than potency. This is because the maximal effectiveness of a drug (efficacy) is generally what determines which drug is chosen to treat a specific condition.
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Potency: |
The dose or concentration of a drug that is required to produce a response of a certain magnitude, usually 50% of the maximal response for that drug. Potency does not matter as much clinically, as the dose can be adjusted to achieve the desired response.
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Therapeutic Range |
to give enough drug so that the concentration of drug in the blood stays above the minimum drug concentration that produces the desirable response, but below the drug concentration that produces a toxic response |
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Drugs undergo five stages or events after administration: |
1. Absorption from the site of administration 2. Distribution to the site of action of the drug 3. Target interaction (i.e. combination with a receptor or other target) 4. Biotransformation 5. Excretion from the body |
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5 factors which contribute to the variability in the observed response among patients:
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1. Genetic factors
2. Environmental factors 3. Other disease states 4. Altered physiological state a. age b. pregnancy 5. Presence of other drugs
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Pharmacokinetics - four processes |
how the body handles drugs 1. Absorption: 2. Distribution 3. Biotransformation 4. Excretion |
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Bioavailability |
the fraction of an administered dose that reaches the systemic circulation (blood) in an active form |
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Routes of drug administration Name the 3 categories and at least 2 examples in each
Which has highest Bioavailability? Which is fastest? |
Enteral 1. Oral 2. Rectal 3. Sublingual and Buccal (fast under tongue) Topical 1. on the skin 2. through the skin 3. Intraocular 4. Intraotic 5. Intranasal 6. Inhalation Parenteral Routes 1. Intravenous (highest Bioavailability, fast) 2. Intramuscular 3. Subcutaneous |
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Absorption (membrane crossing) |
1. Diffusion through aqueous pores
2. Diffusion through lipid
3. Active or carrier mediated transport |
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Drug biotransformation (metabolism) |
the conversion of the drug to a different chemical compound. Divided into phase 1 and 2 reactions |
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Biotransformation Phase 1 |
The purpose of a phase 1 reaction is to add or unmask a functional group on the drug so that the phase 2 reactions can add a large water soluble component, usually glucuronic acid or sulfate, making the product more water soluble for excretion by the kidney. We think of phase 1 reactions as adding a handle to which we can attach a water soluble component. |
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Biotransformation Phase 2 |
Phase 2 reactions add a large water soluble moiety to the product resulting from phase 1 biotransformation, making the metabolite water soluble for excretion by the kidney. |
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half-life of a drug |
the time required for the body to remove 50% of the dose administered. |
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Types of Adverse effects list 7 |
1. Extension of therapeutic effect 2. Unrelated to main drug action 3. Idiosyncrasy 4. Drug allergy 5. Drug dependence and addiction 6. Teratogenesis (Birth defects) 7.
Carcinogenesis and metabolic activation
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New drugs proceeds through three stages: panacea, poison, and pedestrian. Explain: |
1. Panacea: A solution for all difficulties and diseases. When a new drug is first marketed it is thought that the drug is a major new breakthrough in medicine. 2. Poison: After a few months, additional adverse effects usually become apparent, and sales of the drug drop precipitously. The drug is then thought to be a poison. 3. Pedestrian: With the further passage of time, the benefit/risk ratio of the drug is easier to assess and it is realized that the drug is neither a panacea nor a poison, but rather an average drug. |
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TD50 |
the toxic dose 50. The dose that is toxic to 50% of animals. |
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Therapeutic Index |
(TI) = TD50/ED50 Tells you how safe the drug is
When a drug has a low therapeutic index, it is more likely that toxicities will be observed. |
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Drug interactions |
1. Absorption: One drug can affect the absorption of another drug.
a. One drug may combine with a second drug in the stomach or intestine to form a complex that cannot be absorbed into the blood. b. A drug which increases the movements of the intestine may speed the passage of a second drug through the intestine. c. Some drugs seriously hinder the movements of the intestine. 2. Displacement: A second drug may displace the first drug from its binding site on the blood protein. 3. Changes in Liver Handling of Drug 4. Changes in Excretion |
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Drug-food interactions |
Tyramine, which is capable of raising blood pressure, is broken down in the liver by an enzyme known as monoamine oxidase (MAO). one class of drugs used for treatment of certain types of depression are inhibitors of MAO.If a patient is being treated with an MAO inhibitor and consumes a food containing tyramine, the tyramine will not be broken down to inactive products and the blood pressure raising effects of tyramine will be greatly intensified.
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Selective toxicity |
Common examples of selectively toxic agents are herbicides, antibiotics, and anticancer drugs. a drug which exerts a toxic effect on an invading parasite or organism, but not harm the host
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