test 1 Flashcards
1
Q
what is intrinsic
A
from within human beings themselves
2
Q
what is extrinsic
A
determined by environmental factors
3
Q
what is biopharmaceutical agents
A
constitute a group of therapeutic agents that do not fit the traditional definition of drugs.
4
Q
what is the difference between generic names and trade names
A
generic names are recognised internationally, while trade names are unique to the manufacturers of specific medicines
5
Q
what is pharmacodynamics
A
describes the physiological effects that cells have on living cells or organisms and shows how drugs influence body functions through biochemical changes in the body.
6
Q
what is pharmacokinetics
A
Describes the absorption, distribution, metabolism (or biotransformation) and elimination through excretion of drugs and how the body acts on the drugs
7
Q
what is pathology
A
the scientific study of disease and disease-causing factors
8
Q
what is pharmacology
A
the origins and actions of drugs used to manage disease
9
Q
what is pharmacotherapy
A
refers to patients actual drug programme
10
Q
Pharmacotherapy has a reduced role in which treatment modality
A
surgical treatment modality
11
Q
what are examples of biopharmaceutical agents
A
monoclonal antibodies
recombinant human insulin
certain vaccines
clotting factors VIII and IX
enzymes
hormones
cytokines
Examples include infliximab, bevacizumab, rituximab, growth hormone, adalimumab, factor CSF, tissue plasminogen factor
12
Q
what are cytokines
A
a diverse group of signalling proteins primarily produced by the cells of the immune system.
13
Q
a generic name of a pharmaceutical product is…
A
always indicative of the actual drugs in the product
14
Q
Pharmaceutics
A
is the art and the science of drug preparation, design and dosage forms
15
Q
Therapeutic effects
A
the desired effect of a drug
16
Q
side effects
A
effects that occur in addition to those that the drug was meant to elicit
17
Q
toxic effects
A
usually dose dependent and manifested during overdose
18
Q
teratogens
A
that may affect normal embryonic development and can cause recognisable congenital birth defects
19
Q
mutagenic effects
A
mutagens cause genetic defects by affecting developing germ cells
20
Q
Paradoxical drug action
A
a drug reaction that results in the opposite effect to that which was expected.
21
Q
drug dependency
A
an urge to repeatedly use the drug
22
Q
tolerance
A
A need to increase the doasage to achieve the same level of therapeutic effect
23
Q
porphyria
A
a group of disorders that involve the biosynthesis of haem and cause an excessive renal excretion of porphyrins or their precursors
24
Q
for drugs to exert their effects on the body, they need to interact with large complex macromolecules via their
A
receptors
25
what are ligands
ligands are molecules that bind to receptor sites to transmit chemical signals
26
ligand-receptor
ligand-receptor or drug receptor complexes occur once a stable but reversible chemical bond has formed between the two molecules in question
27
specific ligands
neurotransmitters (dopamine, noradrenalin and acetycholine)
hormones (adrenalin, oxytocin and insulin)
autacoids (histamine, seratonin and prostaglandins)
28
specific ligand receptors
drugs that bind to these receptors actually target the binding sites of the normal physiological, signal-transmitting substances that directly.
29
membrane receptors
-these have ligand-binding molecular structures that are found in the outer surface of the cells plasma membrane
examples
-ligand-gated ion channels
-G-protein coupled receptors
-kinase-linked receptors
30
Intracellular receptors
-act as primary target areas for steroids
-these can be cytoplasmic or nuclear
31
enzyme receptors
some drugs interact with enzyme receptors as their targets and consequently inhibit the normal physiological functions of the enzymes in question.
-competitive inhibitors
-non competitive
32
Intracellular receptors are...
specific ligand receptors
33
transport carrier proteins
transport proteins that use facilitated diffusion and active transport of ions and neurotransmitters across plasma membranes
34
structurally specific
-have a 3D structure
-they are therapeutically effective
-changing their chemical structure will have a major influence on their biological activity at the specific receptor sites
35
structurally non specific
- are highly lipid soluble
-do not share similarities in their chemical structure
-require relatively large doses to produce their clinical effects
36
the topical delivery of drugs
applied to specific body surface areas where they exert localised effects
37
absorption
refers to the passage of drug molecules from various mucous membranes skin or subcutaneous tissue into the bloodstream
38
distribution
transport of these molecules via the systemic circulation to the various fluid compartments tissues and organ systems of the body that constitutes their site of action
39
drug absorption
is the movement from their site of administration into the bloodstream
40
what is systemic and topical delivery of drugs
systemically is the various routes used to deliver drugs to the rest of the body
topical delivery of drugs is when drugs are applied to specific body surface areas where they exert localised effects
41
what is absorption
refers to the passage of drug molecules from various mucous membranes, skin or subcutaneous tissue into the bloodstream
42
what is the distribution
refers to the transport of these molecules via the systemic circulation to the various fluid compartments tissues and organ systems of the body that constitute their sites of action
43
Absorption entails the process of a drug molecule moving from the .....
small intestine to the hepatic portal system
44
is sodium ions higher or lower in the extracellular or intracellular fluid
sodium ions are higher in the extracellular fluid
45
is potassium ions higher or lower in the extracellular or intracellular fluid
potassium ions are higher in the intracellular fluid
46
cells typically have the following characteristics
plasma membrane is composed of two layers of phospholipid molecules
47
the cell membrane has the following characteristics
the hydrophobic tails face each other
48
selective permeability means that...
solvents can pass through
49
where are peripheral proteins found
are found on either the inner or outer surface of the membrane
50
integral proteins.....
A) Span the entire thickness of the membrane
B) Are found on the inner surface of the membrane
C) Are involved in signal transduction
D) Are found on the outer surface of the cell membrane
A) Span the entire thickness of the membrane
51
channel proteins
-form small aqueous pores or channels in the membrane
-they serve as passageways for selected polar molecules and ions to cross the membrane
-they need to be extremely small
52
carrier proteins
-are involved in the active tansport of molecules or ions or facilitated exchange diffusion of such particles
-have limited drugs that meet the structural requirements for carrier transport
53
simple passive diffusion
-does not require any cellular energy
-move along from an area of high concentration to a area of low concentration
-small non polar lipid soluble molecules
-polar, water soluble molecules
54
active transport
-requires energy and carriers to move against the concentration gradient
-it uses ATP directly
-it moves from areas of low concentration to high concentration
55
facilitated difusion
-does not require cellular energy
-larger molecules
-needs proteins to diffuse through membrane
56
Physiochemical properties of drugs that facilitate their abilities to cross a cell membrane
-Un-ionised molecules are lipid soluble
-water-soluble drugs that are small enough
57
where do acidic drugs and basic drugs tend to stay in (extracellular or intracellular)
acidic drugs tend to stay in the extracellular fluid
basic drugs tend to stay in the intracellular fluid
58
Psychochemical properties that enable simple passive diffusion of drugs include
-must have a high degree of lipid solubility
59
psychochemical properties of drugs that promote active transport
drugs must bind to actual carrier proteins
60
dissolvability of a drug is influenced by what
lipid solubility of the drug
61
drug absorption is most effective via an absorptive surface area is most effective....
in the small intestine in the prescence of diarrhoea
62
specific biological barriers that are easy for drugs to penetrate include
placenta
63
specific biological barriers that are not easy for drugs to penetrate include
thyroid, brain and prostate
64
when will 100% bioavailability of drug occur
when it is given intravenously
65
drug distribution
movement of drug molecules to their target areas
66
how are drugs distributed
in divided amounts according to the cardiac output that the organs receive
67
the termination of a drug comprises the kinetic processes of
biotransformation and excretion
68
where are volatile drugs most commonly terminated
lungs
69
drugs may be terminated using an
antagonist
70
for drug molecules to be biotransformed in the liver they need to have what characteristics
non polar and lipid soluble
71
a plasma esterase enzyme that is responsible for the biotransformation of water soluble drugs include
cholinesterase
72
what is a pro drug
it is a drug that requires biotransformation into its active metabolise by phase 1 reactions to be effective
73
which drug is cleared by the liver very quickly that is cannot be given orally
lignocaine
74
An organ that is an excretory organ of a particular drug will contain a blood concentration of the drug that is
A Higher than the rest of the body
B Lower than the rest of the body
C The same as the rest of the body
D Unlikely to be toxic
A- Higher than the rest of the body
75
Enterohepatic cycling
conjugated metabolities are hydrolysed to make them lipid soluble again
76
liver excretion of a drug occurs by which process
Conjugation of metabolities
77
drugs that are prepared for excretion by the kidneys are..
ionised so that they wont be reabsorbed
78
Elimination half life
the amount of time that it will take for the drugs plasma concentration to be reduced by 50%
79
zero order kinetics
saturation of the absorption and excretion processes may occur
a constant amount of the drug is eliminated
also referred to as dosage dependent kinetics
80
first order kinetics
a constant fraction of the drug is eliminated per unit time
these drugs will not become saturated
this is also referred to as dosage independent kinetics
81
what are examples of drugs that follow zero order kinetics
heparin
the salicylates
phenytoin
82
what are examples of drugs that follow first order kinetics
amoxicilan
83
a steady state concentration is an example of
takes approx 4 to 5 times the drugs half life to complete
84
the therapeutic index
difference between the minimum plasma concentration at which the drug is effective and the minimum level at which the drug becomes toxic
85
a drug which has a narrow therapeutic margin
has a small therapeutic window
86
a drug which has a broad therapeutic margin has the following characteristic
a small therapeutic window
87
what are examples of membrane receptors
ligand gated ion channels
G protein coupled receptors (GPCR)
Kinase linked receptors
88
what is affinity
may be defined as the tendency or degree to which drug molecules are drawn to their receptors
-provides us with an indication of the strength of the chemical bonds
-the power of attraction between the drug molecule and its receptor
89
organophosphate pesticides are examples of drugs that
are terminated only once new receptor sites are synthesised
90
effect
is an observable result due to a change in biological body processes and the receptor
91
intrinsic activity
describes the biological effectiveness of the drug-receptor complex (the ability of the drug to elicit a cellular response)
is the ability of a drug with an affinity for a specific receptor to stimulate this receptor
the cells may be exhibitory or inhibitory
92
what is a receptor
a receptor is the part of a macromolecular complex in a living cell or living organism with which a drug interacts
93
what is a specific receptor
if stimulated leads to a specific pharmacological effect
94
what is effect
is an observable result owing to a change in biological body processes brought about by drug receptor interaction
95
Biophase
the area directly surrounding the receptor binding site
96
signal transduction
A cascade of cellular events set in motion by receptor binding and then amplified
97
specific ion channels
exhibit selectivity for their specific ions only
98
decreased ion channel permeability occurs when
endogenous substances prevent the channel from opening
99
In intrinsic activity, the active cellular responses to
dopamine-exhibitory
serotonin and dopamine-exhibitory
GABA- inhibitory
100
what is an agonist
these are drugs that have intrinsic activities equal to one and are capable of eliciting maximal cellular responses. they display a strong affinity for its receptors
101
what is a competitive antagonist
drugs that exhibit intrinsic activities of zero. they usually display higher affinities for their receptors than their corresponding agonist. they are also referred to as blockers. these drugs merely block receptors as to prevent agonists
102
Dualists
some drugs are neither full agonists neither competitive antagonists, they may be categorised as partial agonists or agonists-antagonists. they have intrinsic activities ranging between zero and one
103
drugs that are competitive antagonists
are capable of displacing the corresponding agonist from its receptor site
104
Multipotent blockers
drugs that are capable of acting as receptor blockers in more than one receptor system
105
chemical antagonists
forms a chemical bond with the agonist, thereby decreasing its affinity for its receptor binding sites
the concentration and effectivness of the agonist is therefore decreased
examples protamine sulphate, dimercaprol
106
Functional physiological antagonist
is actually an agonist that acts on a different receptor system, where it elicits the opposite physiological effects to those elicited by the initial agonist.
107
Metaffinoid antagonists
change the conformation of the receptor-binding sites utilised by agonists. this implies that the agonist1
108
Most receptors used by drug molecules
can produce a maximal response despite low density of receptors
109
in the autonomic nervous system
neurotransmitters also act as functional or physiological antagonists
110
Biochemical or pharmacokinetic antagonists
a biochemical antagonist directly decreases the concentration of the agonist in the biophase
111
analogues
these are substances that have similar chemical structures, which differ only in respect of a specific component.
112
drugs that target enzyme receptors
can inhibit the activity of the enzyme
113
Tolerance
the dose of a drug must be increased with repeated administration to maintain the same therapeutic effect
114
Synergism
2 drugs added together have a greater effect than the drugs administered separately eg bactrim
115
the adrenergic receptors are stimulated by the
sympathetic nervous system
116
the cholinergic receptors are stimulated by the
parasympathetic nervous system
117
Alpha 1
Alpha 1
excitatory
postsynaptic receptors stimulation of these receptors provide smooth muscle contraction
they are found in the smooth muscles of most arterioles and veins which produces vasoconstriction and increase in arterial blood pressure
the radial muscle of the eye simulation produces dilation of the eye mydriasis
Drugs used
Oxymetazoline (Agonist)
Doxazosin (Antagonist) / Cardura
118
Alpha 2
Alpha 2
inhibitory presynaptic
found on sympathetic neurons, blood platelets and also some postsynaptic tissues
simulation of these receptors decreased cAMP
presynaptic receptors stimulation provides for the inhibition of further noradrenaline release through a negative feedback mechanism simulation in peripheral tissues produces decreased insulin secretion decreased formation of the aqueous humour in the eye and mediation of platelet aggregation. regulation of blood pressure.
Drugs used
Clonidine/Catapress (Agonist)
119
Beta 2
inhibitory
-smooth muscle relaxation
-vasodilation
-bronchodilation
drugs used
salbutamol-agonist
propanolol-antagonist
120
Beta 1
-excitatory
-the heart SA and AV nodes
-heart rate increases
-increase the force of the myocardial contraction, atrial and ventricular excitability and contractibility
-kidneys- increases renin secretion with activation of the RAAS
drugs used
dobutamine- agonist
atenolol- selective antagonist
121
Muscarinic 1 (M1)
-excitatory
-acetylcholine
-found in the CNS, in autonomic ganglia and on post synaptic terminals
-motor coordination, sleep, arousal, memory, processing and awareness
drugs used
atropine- antagonist
metacholine- agonist
122
Muscarinic 2 (M2)
-acetylcholine
-decreases cAMP
-these are found in the supraventricular cardiac tissue, SA and AV node
drugs used
Neostigmine- antagonist-reversal muscle relaxant
123
Nicotinic receptors
-excitatory
-brain and spinal cord
drugs used
varenicline-agonist (nicotine addiction)
124
Dopamine 1
-present of vascular smooth muscle
-increased blood supply to organs
-inhibitory
drugs used
Levodopa (agonists for parkinsons)
125
Dopamine 2
-inhibitory
-they are present on the CNS
-stimulation of these receptors decreases cAMP
drugs used
Metaclopramide- maxolan-antagonist
126
Serotonin (5-HT1)
-decreases cAMP
-may be influenced by the management of anxiety/migraine headaches
-stimulation will result in vasocontriction
-GIT-entero
drugs used
amitriptyline-agonist
clonidine-antagonist
127
Histamine (H1)
-excitatory
-allergic reactions
-itching and angioneurotic oedema
-vasodilation and increased vascular capillary permeability that accompany allergic reactions and inflammation
bronchial smooth muscle contraction
drugs used
citririzine, chlorpheniramine, cyclizine-antagonists
128
Histamine (H2)
-allergic reactions
-facilitate the secretion of gastric acid in the stomach
-increase HR and contractibility
129
Opioid (Mu1)
-endorphins
-CNS- brainstem
-inhibitory
-decrease cAMP
-influence processing of pain and emotions
-causing analgesia euphoria
morphine-agonist- tramadol
naloxone-antagonist
130
Opioid (Mu2)
-endorphins
-CNS- brainstem and GIT
-inhibitory
actions when stimulated
-decrease cAMP
-Influence processing of pain and emotions
-causes constipation and respiratory depression
drugs used
pentazocine-agonist
naloxone-antagonist
131
GABA (Gamma aminobutyric acid)
CNS- cerebellum and basal nuclei
-inhibitory
actions when stimulated
-excitability of neurons
-influences motor coordination
drugs used
propofol-agonist
benzodiapines-agonist
flumazenil-antagonist
