General pharamacology introduction Flashcards

1
Q

Dif of pharmacology

A

is since which deals with drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Dif of drug

A

its a chemical agents used for treatment of diseases or prevention of diseases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

names of drugs?

A

1-chemical name
2- non-propitry name : genetic name referred to a scientist
3-propitry name : commercial name

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

explain the general pharmacology and its parts

A

-its consist of 2 parts :
1-pharmacodynamic : the effect of the drug on the body ( it has two parts :effect and mechanism)

2-pharmacokinetics : the effect of the body on the drug
it has 4 parts which is :
1-absorption
2-distribution
3-metabolism
4-elimination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

explain the pharmacodynamic dynamic

A

-Dif : its the effect of the drug on the body
—once the drug entering the body the drug goes to body control system which is the targets :
1-drug receptor. 2- ion channels
3-enzymes ( extra or intra cellular )
4-transport system ( carrier molecules )

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

explain the receptor and its types

A

-receptor: its protein micro-molecule embedded in the cell membrane has extra cellular level and intra cellular level
-if the drug bind to receptor called ligands , if the ligand activate the receptor will be called agonist , and if blocked or inhibit the receptor called antagonist
—-types of receptor:
1-ligand gated-ion channel :after binding of agonist or antagonist to ion channels receptor the transmembrane conductance of specific ion increased or decreased and that causing a change in vital activity of cell membrane

2-G protein couples receptor :they are located in cell membrane and they implement there responses through the second massinger and when agonist bind to it a further signal performed and change a number of enzymes in cell or coupled ion channel

3- enzyme linked receptor: usually has extra cellular domain for ligand which is cytokines
and intracellular domain which is
tyrosin kinase

4-receptor regulating gene transcription
receptor regulating gene transcription are termed nuclear receptor
some of them located in the cytoplasm and migrate to nucleus only after binding to ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what us the affinity ?

A

is the ability of substance to bind to a biological target resulting of formation of substance- receptor complex

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what is the types of bonds between the drug and receptor?

A

1-hydrogen bond : like OH bond NH and its reversible
2-ionic bond : opposite charge attract each other , and its reversible
3-covalent bond : its sharing of atoms and becomes 1 unite and its irreversible

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

explain the Agonist

A

-agonist: its substance with affinity and intrinsic activity
- the agonist can reach maximum effect which can be expected from the medicinal agent and thats called = efficacy
-another term is the potency: which is determined by the concentration in which the substance produced 50% of the effect

— types of the agonist :
1-full agonist : its the ligand that bind to receptor and produce the maximum cellular response
2-partial agonist : its the ligand which bind to the receptor with internisc activity greater then 0 but less the 100%

— type of response in the agonist
1-graded response : its response proportionally related to the dose which mean increasing of the dose will lead to increase of response
2-quintal response :the response about all or non Ex the epilpicy and arethmeia 

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

explain the antagonist

A

-we have 2 types :
1- comparative antagonist : have affinity but no intrinsic activity ( blocker ) and bind at the same site of agonist

2- non-competitive antagonist : occurs when antagonist occupies which so called allosteric binding site in receptor
(micro molecule non receptor sites which regulate the receptor activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what other types of antagonist?

A

1-chemical antagonist: ex mixing acidic drug with alkaline drug
2-physical antagonist: ex patient have a toxicity of (heparin ) which has negative charge so we give him ( protamine ) which has positive charge so they make complex and the body execrating them both
3-pharmacokinetics antagonist; ex if a patient has anemia and he take medicine for the anemia and then he took a medicine for stomach acid which is ( antacid ) the antacid prevent the absorption of iron which he needed for the anemia so this is a antagonism on level of the absorption

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

how drugs can effect:
1-ion channel
2-enzymes
3-carrie molecules ( transporter )

A

1- ion channels:
1-1 the drug block it physically
1-2 receptor ion channel
1-3 through g-proteins receptor activate it which lead to Camp open the ion channel
——-
2-enzymes:
2-1 the drug goes and bond with enzyme with reversible bond
2-2 irreversible bond like ( Organophosphate)
2-3 false substances: like Ldopa converted to be dopamine, so when the drug interact with the enzyme the enzyme false between the real L dopa and fake L dopa which is the the drug and prevent synthesis of dopamine
———
3- carrie molecules or transporter :
3-1 increase the carrier molecules or decrease it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

explain the therapeutic index

A

-therapeutic index : is commonly used to quantify the therapeutic window
and its Ti = Td50 / Te50
-TD50 : its the dose that produces toxic effects of 50% of population
-Te50: its the dose that produces therapeutic effect of 50% of the population

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what is the medication dose ?

A

its starting from up to down ( healthy to lethal )
1-threshold dose
2-mean therapeutic dose
3-maximum therapeutic dose
4-toxic dose
5- lethal dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

explain the pharmacokinetics: Absorption

A

DF : its the passage of the drug from site of administration to the plasma
— main site of administration:
1-oral. 2-sublingual 3-rectal 4-inhalation 5- injection

—- transmembrane movement of the drug :
1-simple diffusion: the most important method of drug absorption
2-filtration: important for drug excretion by kidney
simple and filtration also known as passive transfer
3-active transport
4-facilitated diffusion:
active and facilitated also known as carrier -mediated
5-pinocytosis: its active process which energy dependent in which the drug is engulfed inside the cell
pinocytosis and facilitated and active known as specialized transporter

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q
  • factors effect the drug absorption
A
  • there is 2 types of factors
    1- factors related to the drug :
    1-1 molecular size
    1-2 dose : increase of the dose lead to increase of the absorption
    1-3 lipid salability ( pKa) : drug ionization

2- factors related to the body :
2-1 route of administration
2-2 integrity of the absorption surface
2-3 blood flow

17
Q

explain the The Henderson-Hasselbach Equation ( pKa)

A

— The Henderson-Hasselbach Equationexpresses a relationship between the body compartment pH, the drug’s pKa (can be measured in the laboratory), and provides the ratio of acidic and basic forms of the drug

  • clinical significant for pKa:
    1- know the site of drug absorption from GIT
    2-treatment of toxicity, with acidification or alkalization
18
Q

explain the ion trap : aspirin

A
  • the ion trap is mean that the drug will ionized in the cell and cant diffuse to the blood stream
    -Ex: ion trap for aspirin
    the ph pKa for aspirin is 3,5
    ph of stomach is 1,5
    ph of stomach cell same as plasma witch is 7,4
  • so if patient to a large dose of aspirin with empty stomach the aspirin will move to stomach and bcs both acidic the aspirin will diffuse to stomach cells but becs the stomach cells doesn’t change the ph bcs there is no food could explode , and the patient start vomiting blood , but after a time the ionized aspirin will change chimcailly and get diffused to blood circulation
19
Q

explain the pharmacokinetics: distribution Vd

A

1— volume of distribution (vd)
Df: the apparent volume if water into which the drug is distributed in the body after distribution equilibrium

  • site of drug distribution:
    1- plasma 3 L water
    2- extracellular 9L water
    3-intercellular 29 L water
    total 41-42 L water in the whole body
    -formula: vd=total amount of drug divided by plasma concentration
    —- clinical significant :
    we can know if the patient can be treated with dialysis or not
    1- so if its vd less then 5 L it can be dialysis
    2- if between 10-15 L its restricted to medical stuff to decide
    3 if its more then 41 L then the drug is more bounded to proteins tissue and cannot be removed by dialysis
20
Q

explain the pharmacokinetics: distribution proteins bound

A
  • Df of binding of the drug to plasma proteins: most drug inter the body are bound to plasma proteins, albumin the most important plasma proteins beca can bind with positive and negative charge drug
  • clinical significant : the pharmacological effect of the drug is related only to free part of the drug not the part which bound to plasma proteins
    , the part that bound to plasma proteins work as reservoir from which the drug slowly realized
21
Q

explain the pharmacokinetics: metabolism

A

—Df of metabolism and its main function: transfer the substance that entered the body which is lipid-soluble to water-soluble to be easy excreted
—- the major site of metabolism is the : liver but not the only
——- ceases of drug in the metabolism is 1 of these 4 :
1- active to inactive
2- active to active ex: codein to morphen
3-inactive to active : ex enaloprel to enalaprolant
4- from any shape to toxic: ex paracetamol to inAcitlypenzokinon

22
Q

explain the pharmacokinetics: metabolism Phase 1

A
  • it has 3 types :
    1-oxidation ( the important one )
    2-reduction
    3-hydrolysis
    —-Phase 1 oxidation :
    happend in the vesicles inside the hepatocytes there is a lot of enzymes group but we are interested in 1 group of them which call ( cytochrome P450 )
    its family of enzyme consist of not less then 50 enzyme which is mixed function oxignesis
    —- the most valuable enzyme of this family called (CYP3A4) this enzyme can metabolize 50% of the our drugs
    —types of microsomal :
    1- microsomal inducers : induce the cyp3a4
    1-1 barbiturates
    1-2 Rifampin
    1-3 carbamezoampin
    1-4 cigarettes soaking
    2- microsomal inhibitors: inhibit CYP3A4
    2-1cimatadene
    2-2 ketokonzol
    2-3 Erythromycin
    2-4 grape fruit

——- Ex the contrasptive bills with cigarettes smoking or rifampin

23
Q

explain the pharmacokinetics: metabolism Phase 2

A

-Phase 2 ( conjugated ) : phase 2 activated if chemistry of the drug doesn’t work with phase 1
— mechanism:
if the liver fail to metabolize with first phase , the liver will conjugate the drug with large molecules like acytlation , sulfation but most of the time glucroinc acid , in neonates the primary pathway is sulfation , after conjugated with large molecule which is water-soluble the liver will excrete the conjugated molecule through bile then to intestine

—- enzyme inducer or inhibitor : its only available with ( groconail transfers )

24
Q

explain the pharmacokinetics: metabolism : first pass metabolism

A

Df : the first place at which drug could be metabolize partly before reaching the systemic circulation
—- cases of First pass metabolism:
1-passing through the liver without in first pass metabolism
2- frist pass metabolism of drug partly in the live
3- the liver first metabolize the drug
100 % ex ledokine ( we should look for another rout of administration)

25
Q

what is the Bioavailability?

A
  • its the fraction of the drug that reach the systemic circulation after passing the ( absorption and first pass metabolism )
  • formula:
    bioavailability=absorption - FPM
    result by percentage
26
Q

explain the pharmacokinetics: Elimination

A
  • elimination = excretion + metabolism
    Clearance (Cl, ml/min.) – volume of blood plasma which totally cleared of drug per unit of time
    Cl total = Clrenal + Clhepatic + Clother
    – Most drugs are eliminated by first-order process. The amount of drug eliminated per unit of time does not remain constant. But fraction of drug eliminated per unit of time remains constant
    Half-life – time necessary for the concentration of drug in the plasma to decrease by half
27
Q

what is the half life and when the drug is eliminated ?

A

Half-life – time necessary for the concentration of drug in the plasma to decrease by half
– drug eliminated after 4-5 half life

28
Q

what the best describes a lipophobic drug?

A

It always requires an active process for transport.

29
Q

Which drug characteristic makes a drug more likely to enter a cell through a protein channel?

A

Water soluble drug

30
Q

Which parameter change will lead to an increase in passive diffusion into a cell?

A

Increased surface area

31
Q

A lipophiliic drug is

A

is usually nonpolarized.

32
Q

A 5 year old child overdoses on her mother’s anti depression medications (weak acid). The pKa of the drug is 3.9. The pH of the small bowel is 5.9. What percentage of the drug is potentially absorbable across the lipid membrane?

A

1%

33
Q

A patient has overdosed on pyrimethamine (weak bases), with a pKa of 7.42. What percentage of the drug will be trapped in the urine if the urine pH is 5.42?

A

99%

34
Q

A patient has overdosed on pyrimethamine. It has a pKa of 7.42. What portion of the drug will be hydrophilic at a urine pH of 8.42?

A

10%

35
Q

A 44 year old woman presents to the hospital ER with a low blood pressure of 77/40, a heart rate of 40, and normal pupils. She has an empty bottle of blood pressure pills that have a pKa of 7.5 (weak base). In addition to hemodynamically supporting the patient, you want the patient to excrete the drug in the urine. Theoretically, of the following choices, what would be the most appropriate action?

A

Acidify the urine. This will protonate the drug, allowing it to be more soluble in the urine.

36
Q

A competitive inhibitor will:

A

act at the same site as the ligand.