Created by Ayman Barghout
over 8 years ago
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Question | Answer |
Biological screening | Qualitative process in which an unknown drug's biological effect or mechanism of action is determined |
Biological assays | Quantitative process in which a known drug's concentration, potency or LD50 is determined |
Methods of developing new drugs | 1. Purification & Extraction of natural drugs. 2. Chemical synthesis of new drugs. 3. Modification of chemical structure of existing drugs. |
Reasons for modification of chemical structure of existing drugs | 1. Improve selectivity of drugs. 2. modify absorption - distribution or elimination. 3. Decrease the cost of the drug |
Types of screening | Simple and blind |
Simple screening | Detecting the action of a drug with expected pharmacological activity. e.g. testing the hypoglycemic effect of a derivative of sulphonylurea or metformin. |
Blind screening | Determining the biological effect of a newly synthesized drug |
Blind screening tests | Primary screening : Neuropharmacological tests. Secondary screening : in-vitro and in-vivo tests |
Primary screening vs. secondary screening | Not specific (predicts) vs. specific (confirms) |
Neuropharmacological tests | 1. Behavioural responses. 2. Neurological responses. 3. Autonomic responses |
Neuropharmacological tests : Behavioural responses | 1. Awareness. 2. Mood. 3. Motor activity |
Behavioural responses: Awareness | 1. Consciousness. 2. Visual placing (righting reflex). 3. Stereotypy. 4. Passivity. |
Awareness : Consciousness | Alertness → CNS stimulation Stupor → CNS depression |
Awareness : Visual placing (Righting reflex) | Decreased righting reflex → muscles relaxation or CNS depression |
Awareness : Stereotypy | In mice Circular movements → Morphine Searching movements of the head → Amphetamine |
Awareness : Passivity | Indication of CNS depression, muscles relaxation or paralysis |
Behavioural responses : Mood | 1. Grooming. 2. Vocalization. 3. Restlessness. |
Mood : Grooming | Increased grooming → CNS or sympathetic stimulation |
Mood : Vocalization | Indicates painful stimulation ( algesic or noxious stimuli) |
Mood : Restlessness | Indicates CNS stimulation or approach of convulsions |
Behavioural responses : Motor activity | 1. Spontaneous activity. 2. Reactivity. 3. Touch responses. 4. Pain responses. |
Motor activity : Spontaneous activity | Increased activity → CNS stimulation Decreased activity →CNS depression |
Motor activity: Reactivity | How reactive the animal is to changing his environment |
Motor activity : Touch responses | Amphetamine → increases touch response → mouse jumps upon being touched |
Motor activity : Pain response | Reduced pain response →CNS depression or analgesia |
Neuropharmacological tests : Neurological responses | 1. Reflexes. 2. CNS stimulation. 3. Muscle coordination. 4. Grip strength. |
Neuropharmacological tests : Autonomic responses | 1. Optical signs. 2. Secretory signs. 3. General signs. |
Autonomic responses : Optical signs | 1. Mydriasis vs Miosis. 2. Palpebral opening (opening of eyelids). 3. Exophthalmos (Protrusion of eyeball). |
Autonomic responses : Secretory signs | SLUD → Parasympathomimetic (Muscarinic activity) Note: SLUD = Salivation, Lacrimation, Urination and Diarrhea. |
Autonomic responses : General signs | 1. Writhing. 2. Piloerection. 3. Hypothermia. 4. Skin colour (red or white). 5. Heart rate. 6. Respiratory rate. |
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