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Pharm final exam
Pharm Alice 6-9 Andy 5-7
| Question | Answer |
|---|---|
| What are the three main fluid compartments in the body? | Extracellular, intracellular and transcellular |
| What is intracellular fluid composed of? | The sum of the fluid content inside all the cells in the body |
| What is extracellular fluid composed of? | Blood plasma, interstitial fluid and lymph |
| What is transcellular fluid composed of? | The cerebrospinal, intraocular, peritoneal, pleural, synovial and digestive secretions |
| What type of drug molecules may be pharmacologically active? | Unbound drugs |
| What structures/tissues can drug molecules bind to? | Body fat and plasma proteins |
| What plasma protein is used in drug binding? | Albumin |
| What is the definition of volume of distribution? | The volume of fluid in which the dose of drug would theoretically have to be diluted to produce observed drug concentration in plasma |
| What is the equation for Vd? | Vd= dose/ plasms concentration |
| What are the practical used for Vd? | Tells us how much of a drug needs to be added to the body to achieve a specified concentration in the sampled fluid and the magnitude of the value indicates where the drug is stored or found in the body |
| What is drug elimination? | The irreversible loss of drug from the body that occurs via metabolism and excretion |
| What is the definition of metabolism? | Enzymatic conversion of one chemical entity to another by the process of biotransformation |
| What is the definition of excretion? | Removal from the body of chemically unchanged drug or its metabolites via the kidneys |
| Why cant the kidneys eliminate lipophilic molecules efficiently? | Because the molecules must be first metabolised into more polar products before excreted |
| What is a prodrug? | A drug administered in an inactive or slightly less active form |
| What are some examples of pro drugs? | Aspirin, codeine and L-dopa |
| Where are metabolising enzymes found in the liver? | The smooth ER and mitochondria of hepatocytes |
| What is hydroxylation? | When oxygen is incorporated into the drug molecule |
| What is oxidative deamination? | Oxidation causes the loss of part of the drug molecule |
| What type of enzymes are involved in phase 1 metabolism? | Cytochrome P450 |
| How do the P450 enzymes differ? | By amino acid sequence, their regulation by inhibitors and inducing agents and the specificity of the reactions that they catalase |
| What is the overall net effect of reaction of the CYP450 drug oxidation process? | The addition of one atom of oxygen to the drug to form a hydroxyl group while the other atom of oxygen is converted to water |
| What groups of substrates are used in conjugate formation? | Glucuronic acid, sulfate, methyl, acetate and glutathione |
| Where does filtration occur in the nephron? | The renal corpuscle |
| What is the definition of filtration? | A passive process that permits of prevents movement across a barrier based on solute size |
| What does secretion involve? | The transport of solutes from blood across tubular epithelium and into tubular fluid |
| What are the three processes that account for renal drug excretion? | Glomerular filtration, tubular reabsorption and active tubular secretion |
| What is the normal glomerular filtration rate? | 90-120 ml/min |
| What is glomerular filtration rate? | The amount of filtrate formed per unit time |
| What is ion trapping? | The build-up of a higher concentration of a chemical across a cell membrane due to the pKa value of the chemical and difference of pH across the cell membrane |
| What is the formula for clearance? | CL=VdxK |
| What factors effect the rate of drug elimination? | Vd of drug, degree of protein binding of drug, glomerular filtration rate and tubular fluid pH |
| What are the symptoms of Parkinson's? | Tremor at rest, muscle rigidity, hypokinesia, slowed movement and dementia |
| What are the causes of PD? | Stroke, viral, drug induced, environmental toxin, gene mutations and trauma |
| What is PD associated with in terms of neurons? | Loss of dopaminergic neurons from the substantia nigra region of the brain |
| What is the substantia nigra in control of? | Co-ordination of movement |
| Why is PD considered a disorder of the basal ganglia? | Because the major projection from the substantia nigra is to nuclei of the basal ganglia |
| What happens when inactive dopaminergic neurons build-up? | Lewy bodies form |
| What protein is present in Lewy bodies? | Mutated alpha-synuclein |
| What is the role of dopamine? | A neurotransmitter that transmits chemical messages from one nerve cell to another across a synapse |
| What enzymes break down and inactivate dopamine? | MAO and COMT |
| What is the main aim of PD drug therapy? | To replace the deficiency of dopamine in the basal ganglia |
| Does exogenous dopamine cross the blood brain barrier? | No, but its precursor levodopa does |
| What is the function of Levodopa in the brain? | To permeate the striatal tissue of the basal ganglia |
| What happens to levodopa in the brain? | It is decarboxylated to dopamine by DOPA decarboxylase enzyme |
| What does carbidopa do? | Prevents levodopa from being converted to dopamine in the periphery in order to reduce side effects |
| What are the side effects of Sinemet? | Involuntary writhing movements, nausea and symptoms of schizophrenia |
| What is the bioavailability of Sinemet levodopa? | 30% |
| What is the half=life of levodopa in the presence of carbidopa? | 1.5 hours |
| Name one dopamine agonist | Bromocriptine |
| What is affinity used to describe? | How avidly a drug binds to its receptor |
| What is the definition of efficacy? | How well a drug/ligand activates a receptor |
| What is EC50? | Concentration of drug that incites half of its maximal effect |
| What is the relationship between potency and EC50? | They are inversely proportional |
| What is occupancy theory? | The magnitude of a response was directly proportional to the amount of a drug bound to its receptor and that maximum response would be the consequence of complete occupancy |
| What is the median lethal dose (LD50)? | The dose of a test substance that is lethal for 50% of animals in a dose group |
| What is the function of LD50? | To evaluate the adverse effects that occur following exposure to a dose |
| What are the three R's of toxicology? | Reduction, refinement and replacement |
| What happens if a compound is too polar? | It may not be absorbed through gut wall due to lack of membrane solubility |
| What compound is used to test lipophilicity? | Octan-1-ol |
| What is the partition co-efficient? | The ratio of how much drug partitions into water and how much partitions into octan-1-ol |
| When is LogP measured? | When the drug is completely un-ionised |
| What is the ideal LogP for a drug to be balanced? | Between 0 and 3 |
| What is ionisation? | The protonation or deprotonation resulting in charged molecules |
| What is pKa? | A measure of the strength of the acid |
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tarajdaly16
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