[PHARM 5] DDD Module 1

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Medicine

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80 Terms

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black bile yellow bile blood phlegm
- framework of health and disease
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Lind 1973
Control of scurvy
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Jenner 1798
Vaccination
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Semmelweis 1861
Surgical infections using aseptic techniques
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1864
British Pharmacopeia
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Rudolf Virchow
Cell theory
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Rudolf Buccheim
Birth of Pharmacology as a scientific discipline
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Magendie and Claude
Therapeutics
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Louis Pasteur
- Germ theory of disease
- Airborne infection was the underlying cause
- Immunization procedures
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Paul Ehrlich
Chemotherapy
- "Vital staining"
- Receptor and Magic bullet
- Antitoxin and bacteria
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Diethyl ether 1950
Sweet oil of vitriol
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Nitrous oxide
* Stupefying agent
* Anesthetic
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Amyl nitrite
* 1st therapeutic drug to come from synthetic chemistry (Gunthrie, 1859)
* Vasodilating effects (Brunton, 1864)
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Aniline
* Precursor of mauvein
* Accidental discovery by Perkin for supposedly Quinine, 1865
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kekule 1865
benzene
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morphine
first alkaloid
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merck
* first local apothecary in 1827
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Scheringer and Boehringer
* 19th century
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squibb
ether (main product in 1858)
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Parke Davis and Eli lilly
* manufacturing chemists, purified Adrenaline
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Bayer Hoechst Agfa Sandoz Geigy
* dyestuff manufacturers
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Chloral hydrate
* first non-volatile CNS depressant
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Barbitone
* by Von Mering
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procaine
* by Einthorn; first local anesthetic drug
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Cocaine
* local anesthetic action in the eye; Simund Freud
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synthetic chemistry
* Became the established model in the early part of the 20th century
* Key discipline in drug discovery; prevailed for 50 years ·
* Research management was largely at hand of the chemists
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benozdiazepines tranquilizers antiepileptic drugs antihypertensive antipshychotics
drugs produced
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natural product chemistry
* Pharmaceutical companies on "love-hate" relationship
* Pharmaceutical industry has difficulty in synthesizing structures.
* Natural products remain significant source of drugs.
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penicillin
1929
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chloramphenicol
1947
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tetracycline
1948
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streptomycin
1949
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vincristine and vinblastine
1958
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paclitaxel
1971
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ciclosporin
1972
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tacrolimus
1993
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mevastatin
1976
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target-driven drug discovery
* Concept of Chemotherapy
* Paul Ehrlich is the first "modernist" who defined the principles of drug specificity in terms of specific interaction between a drug molecule and a target molecule.
* "Corpora non agunt nisi fixata"
* Chemistry remained empiric for many years.
* "Magic bullet"
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IG Farbenindustrie
* interest in preparing antimicrobial drugs
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Prontosil
* saved life of Domagk's daughter
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antimetabolite principles
* By Hitching and Elions in 1944
* Interest in the synthesis of folic acid, purines and pyrimidines as chemotherapeutic agents
* Identified dihydrofolate reductase which is necessary for DNA synthesis.
* Pyrimidine analogues inhibited the enzyme
* Emergent drugs include: Pyrimethamine, Trimethoprim, 6- mercaptopurine, Azathioprine, Aciclovir, Zidovudine
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ligand-receptor interaction
* Drug antagonism
* Classes of receptors have varied effects
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pronethalol
1960 toxic
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propranolol
1964
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burimamide
1972
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digitalis
treating dropsy
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quinine
antidysrhythmic
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amphetamine
adhd
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phenothiazine
laborit's discovery
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promethazine
sedation
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1900
* System of "prescription only" medicines
* What info should be on the label; system of "what cures"
* Controlling of addictive substances
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1937
* Diethylene glycol caused death; demonstrated the need for safety
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1960
* Thalidomide disaster
* Chemie Grunenthal
* UK began to follow US regulatory laws in safety; urgent reappraisal because of the incident
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1963
* Etablishment of Commission on the Safety of Drugs o
* All new drugs has to be submitted for approval before clinical trials and market release
* Medicines Act (closed the loophole) - added efficacy
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Warfarin
- Anticoagulant
- Synthetic compound from dicoumarol
- Found in spoiled sweet clover
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Heparin
- Anticoagulant
- Occurring naturally in mammalian tissues
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Hirudin
- Anticoagulant from leech
- Now produced by genetic engineering
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Opiates
- Analgesic compounds from poppies
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Methylxanthines
- Caffeine and Theophylline
- Phosphodiesterase inhibitors and adenosine receptor antagonists
- Produced by tea, coffee, coca plants
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Statins
- HMG CoA reductase inhibitors used to reduce plasma cholesterol
- Lovastatin is a fungal metabolite
- Later compounds (mevastatin, pravastatin) synthesized from lovastatin
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Cromoglycate
- Asthma prophylaxis
- Synthetic compound based on khellin, plant for herbal medicine
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Vinca alkaloids
- Vincristine and Vinblastine
- Anticancer drugs produced by plants of the periwinkle family
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Paclitaxel
- Anticancer drug from yew tree
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Etoposide
- Anticancer drug synthesized from podophyllotoxin, produced by mandrake plant, used in folk medicine
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Artemether
- Antimalarial drug
- Semisynthetic derivative of artemisinin, a chinese herb
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Ivermectin
- Antihelminthic drug
- Semisynthetic derivative of avermectin, a fungal metabolite
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Antibiotics
- Too numerous to list
- Majority of current antibiotics are derived from fungal metabolites
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Disease genes
* Gene mutations of which cause or predispose to the development of human disease.
* Concept of "inborn errors of metabolism"
* This class of disease genes does not seem to include many obvious drug targets.
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disease-modifying genes
* These are non-mutated genes that are directly involved in the pathophysiological pathway leading to the disease phenotype.
* The phenotype may be associated with over or underactivity of the gene product detectable by expression profiling.
* This is the most important category in relation to drug targets as therapeutic drug action generally occurs by changing the activity of functional proteins, whether or not disease alters their expression level
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gene expression profiling
* Principle: development of any disease phenotype involves changes in gene expression in cells and tissues involved.
* "Critical path genes" may represent potential drug targets, some are "bystander genes" How to identify using this method: group genes into functional classes, then determine plausibility criterion in causing a disease; identify genes which are co-regulated and might point to a biochemical signaling
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comprehensive gene knockout screening
* Elimination or inactivation of the gene
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druggable genes
* For a gene product to serve as drug target, it must possess a recognition site capable of binding small molecules.
* They likely to possess a binding site irrespective of whether such interaction will have a therapeutic value
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combine druggability with disease modifying properties
goal for genes
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target validation
* It refers to the experimental approaches by which a potential drug target can be tested and given further credibility.
* Main approaches are pharmacologic and genetic
* Lack of efficacy causes abandonment of roughly 1/3 of drugs in Phase II, reflecting unreliability of the earlier evidence for target validity
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Pharmacologic criterion
* Whether drugs that influence potential drug target actually produce the expected effects on cells, tissues or whole animals.
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Genetic criterion
* Whether genes are critical to the disease process
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phase 1
safety
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phase 2
efficacy
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phase 3
safety and efficacy in a population
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phase 4
post-marketing surveillance