Pharmacokinetics refers to what the body does to a drug after administration. It involves four key processes: absorption, distribution, metabolism, and excretion. Absorption determines the rate and extent to which a drug enters systemic circulation. Distribution describes a drug's movement into tissues. Metabolism makes drugs more polar and excretable, often by the liver. Excretion eliminates drugs from the body. Together these processes determine a drug's effects over time. Pharmacokinetic concepts help optimize dosing to achieve therapeutic drug concentrations.
Once a drug has gained access to the bloodstream,
it gets distributed to other tissues that initially
had no drug, concentration gradient being in the
direction of plasma to tissues. T
Once a drug has gained access to the bloodstream,
it gets distributed to other tissues that initially
had no drug, concentration gradient being in the
direction of plasma to tissues. T
What Is Disposition?
What Is Distribution?
Steps In Drug Distribution
Factors Affecting Distribution Of Drugs
Physiological Barriers To Distribution
Volume Of Distribution
Specific Tracers Or Markers
Methods For Studying Drug Distribution Pattern
D M Brahmankar and Sunil B.Jaiswal Biopharmaceutics and Pharmacokinetics A Treatise
ADME: the Absorption, Distribution, Metabolism, and Excretion of DrugsRobert T Fremeau Jr PHD
Robert T. Fremeau Jr., PhD, possesses over 20 years of experience in the field of drug discovery in academic and industrial settings. As managing director of NeuroRX Consulting, Robert T. Fremeau Jr., PhD, offers consultation services to pharmaceutical and drug development companies regarding a variety of subjects, including matters associated with pharmacokinetics, the study of how the body processes drugs. Dr. Fremeau can be reached by email at rfremeau@neurorxconsulting.com.
What Is Disposition?
What Is Distribution?
Steps In Drug Distribution
Factors Affecting Distribution Of Drugs
Physiological Barriers To Distribution
Volume Of Distribution
Specific Tracers Or Markers
Methods For Studying Drug Distribution Pattern
D M Brahmankar and Sunil B.Jaiswal Biopharmaceutics and Pharmacokinetics A Treatise
ADME: the Absorption, Distribution, Metabolism, and Excretion of DrugsRobert T Fremeau Jr PHD
Robert T. Fremeau Jr., PhD, possesses over 20 years of experience in the field of drug discovery in academic and industrial settings. As managing director of NeuroRX Consulting, Robert T. Fremeau Jr., PhD, offers consultation services to pharmaceutical and drug development companies regarding a variety of subjects, including matters associated with pharmacokinetics, the study of how the body processes drugs. Dr. Fremeau can be reached by email at rfremeau@neurorxconsulting.com.
ADME is the abbreviation for Absorption, Distribution, Metabolism and Excretion. ADME studies are designed to investigate how a chemical (e.g. a drug compound) is processed by a living organism. Toxicology tests are often a part of this process, yielding the acronym ADMET.
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Anti ulcer drugs and their Advance pharmacology ||
Anti-ulcer drugs are medications used to prevent and treat ulcers in the stomach and upper part of the small intestine (duodenal ulcers). These ulcers are often caused by an imbalance between stomach acid and the mucosal lining, which protects the stomach lining.
||Scope: Overview of various classes of anti-ulcer drugs, their mechanisms of action, indications, side effects, and clinical considerations.
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
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6. Absorption
of drugs:
Transfer of the from the
site of administration to
the blood stream The
rate and extent of
absorption depend on :
• Environmental of drug
absorbed
• Chemical characters of drug
• Rout of administration
7. A) Mechanism of
absorption
of drugs from GIT
Passive diffusion
Drug transfer from high concentration to low
concentration
Don't involve carrier , is not saturable
Majority of drugs are absorbed by this mechanism
11. Factors
Influencing
absorption
Blood flow to the
absorption site :
Intestine receive much
more blood than stomach
so intestine is favored
over the stomach.
Total surface area
available for absorption:
Surface rich in Brush
borders containing
microvilli Intestine has
surface area about 1000
fold Making absorption of
drug across the intestine
more efficient
Expression of P-
glycoprotein :
is transmembrane
transporter protein
responsible for
transporting molecules
including drugs.
12. B) Bioavailability (F)
Rate and extent to which an administered
drug reaches the systemic circulation
Example :
bioavailability of digoxin is estimated to be
0.7 or orally administered tablets , 250
mcg (0.25 mg) o digoxin is given orally, the
effective or absorbed dose can be
calculated by multiplying the administered
dose by F
Amount of drug absorbed = (f) ( dose )
= (0.7) ( 250) = 125mg
13. Factors that influence
bioavailability:
I. First pass hepatic metabolism :
• Drug enter the portal circulation before entering the
systemic circulation . if the drug is metabolized by liver or
gut wall during this initial passage , the amount of
unchanged drug entered circulation is decreased
• First pass metabolism by intestine or liver limits efficacy
of many oral medication
• {For example 90% of nitroglycerine is cleared during first
metabolism so it is administered by sublingual ,
transdermal , intravenous route }
14. Factors
that influenc
e bioavailabil
ity
2) Chemical instability :
Some drug like Penicillin G are unstable in the pH of gastric content
, Others such as insulin are destroyed in GIT by degradative enzyme
3) Solubility of the drug:
Very hydrophilic drugs are poorly absorbed because the inability
to cross lipid rich cell membranes .Paradoxically drugs lipophilic
are poorly absorbed because they are insoluble in aqueous body
fluid cannot gain access to the surface of the cells
4) Nature of drug formulation :
Drug absorption may be alter by other aspects .Particle size Salt
Form Crystal polymorphism Enteric coatings Excepients
15. I.Drug Distributi
-on
• Cardiac output
• Local blood flow
• capillary permeability
• Tissue volume
• degree of binding of drug to plasma and tissue
• lipophilicity
Drugs reversely leaves blood
stream and enter to
extracellular fluid and tissue
for drugs administered IV
absorption is not factor the
initial phase is distribution
phase , it is depend on
18. In brain , capillary structure are continuous and
there are no slit junction. To enter the brain the
drugs pass through endothelial cells of CNS
capillaries or undergo active transport
Example :
levodopa lipid soluble drugs readily
penetrate the CNS because they dissolve
in endothelial cell membrane
By contrast , ionized or polar drugs are generally failed to enter
CNS because they cannot pass through endothelial cell that
have no slit junction
21. Factors
affecting drug distribution?
Binding to tissue proteins :
Acrolein the metabolite of CP * Cyclophosphamide* can cause
hemorrgaic cystitis because of accumulation in bladder.
27. Distribution into the water
compartments in the body:
• Total body fluid :
(Larger Vd indicates greater distribution into tissue; a smaller Vd suggest
confinement to plasma or extracellular
)
28. Effect of Vd
on drug
half-life:
Vd has an important influence on
the half-life of a drug, because drug
elimination depends on the amount
of drug delivered to the liver or
kidney (or other organs where
metabolism occurs) per unit of time.
Delivery of drug to the organs of
elimination depends not only on
blood flow but also on the fraction
of drug in the plasma.
29. Effect of
Vd on
drug half-
life:
If a drug has a large Vd, most of the drug is in the
extraplasmic space and is unavailable to the excretory
organs. Therefore, any factor that increases Vd
can increase the half-
life and extend the duration of action of the drug.
[Note: An exceptionally large Vd indicates considerable
sequestration of the drug in some tissues or
compartments.]
31. Drug
clearance t
hrough met
abolism:
Once the drug enters body the
process of elimination begins.
There are three major route
elimination are hepatic metabolism
, bililary elimination and urinary
excretion.
Elimination is irreversible removal
of drug from body it
involves biotransformation (drug
metabolism ) and excretion.
32. Drug
clearance t
hrough met
abolism:
Excretion is removal of intact
drug from the body theses
elimination process decrease
plasma concentration
exponentially
Metabolism results inproducts
with increased polarity , which
allows the drug to be eliminated
Clearance estimates the volume
of the blood from which the
drug is cleared per unit of time
33. Total CL is a composite estimate
reflecting all mechanisms of drug
elimination and is calculated as
follows :
CL = 0.693*Vd /t1/2
t1/2 half life
34. A) Kinetic
metabolism
The fundamental difference between zero and
first-order kinetics is their elimination rate
compared to total plasma concentration.
38. Reaction
of
metabolis
m
The kideny cannot effeciantly excrete lipophilic
drugs that readily cross dell membranes and
are reabsorbed in the distal
convulated tubules.
Therefor lipid soluble agents are first
metabolized into more polar (hydrophilic)
substanses in the liver via two general sets of
reactions called
Phase 1
Phase 2
39. Phase One
• Converted lipophilic drugs into more polar molecules by
introducing or unmasking a polar function such as –OH , -NH2
. involve reduction , oxidation or hydrolysis
• Phase one may be increase or decrease , have no effect on
pharmacologic activity
• There are two type of phase one :
Phase one utilizing the P450 system
Phase one not involve P450 system
40. Phase I utilizing the P450
system :
• The phase I reactions most frequently
involved in drug metabolism are
catalyzed by cytochrome 450
• P450 is important to cataylze
endogenouse Cpd like (Steriods and
lipids ) and for biotransformation
exogeonus substances ( drugs ,
carcinogens )
41. Phase I reactions not
involving the p450 system
• These include include amine oxidation ( for
example , oxidation of catechole -amine or
histamine) , alcohol dehydrogeneration ( for
example , ethanol oxidation ) estrase ( for
example , metabolism of aspirin n the liver ),
hudrolysis ( for example procaine)
42. Phase II
A subsequent conjugation reaction with an endogenous substrate, such as
glucuronic acid, sulfuric acid, acetic acid, or an amino acid, results in
polar, usually more water-
soluble compounds that are often therapeutically inactive.
44. Renal elimination of a
drug :
1) Glomerular filtration
2) Proximal Tubular
secretion
3) Distal tubular
reabsorption
45. Excretion by
Other Routes:
1)
Drug excretion may also occur via the intestine
, bile, lungs, and breast milk, among others.
2) Drugs that are not absorbed after oral
administration or drugs that are secreted directly
into the intestines or into bile are excreted in
the feces.
46. Excretion by Other Routes
3) The lungs are primarily involved in the elimination of anesthetic gases
(for example, desflurane). Elimination of drugs in breast milk may expose
the breast-feeding infant to medications and/or metabolites being taken by
the mother and is a potential source of undesirable side effects to the infant.
47. Total body (systemic)
clearance
• CL total is the sum of all clearances from the drug-
metabolizing and drug eliminating organs. The kidney
is often the major organ of excretion. The liver also
contributes to drug clearance through metabolism
and/or excretion into the bile.
• Total clearance is calculated using the following
equation:
• CL= CL hepatic +CL renal + CL pulmonary + Cl other
• where CL hepatic+ CL renal are typically the most
important
Click to add text
49. One Compartmental Model
When the drug is rapidly distributed to all parts of the
body, the body is considered behaving as
one compartment, and the drug follows the one-
compartment model
50. Two Compartmental Model
While when the drug distribution to
some organs is faster than
its distribution to other
organs, the body behaves as
two different compartments, and
the drug follows the two-compartment
model.
1= central ( blood and well perfused
organs) * liver , kideny*
2= peripheral ( poorly perfused tissue
)
* muscle *
52. Three parameters
affecting on
Pharmacodynamics
Exposure :
is related to a measure of drug
amount at a particular site in the
body from which it elicits a response.
Commonly used exposure measures
are dose of a drug and plasma
concentrations (Cp)
53. Three
parameters affecting
on Pharmacodynamics
Response
A response (R)refers to a direct measure of
the pharmacologic observation. For example,
measure of diastolic blood pressure (DBP) at
some time point is considered as a
response.
R(t) = Response at time, t :Diastolic blood
pressure
54. Three para
meters affe
cting on Ph
armacodyn
amics
Effect
Effect, refers to a change in the biological response
from one time to another. In other words, an effect is a
derived or calculated value from an observed
response. For example, change from baseline in
diastolic blood pressure is the effect.
E= Effect :Change from baseline in DBP at 8 weeks
To further illustrate, let us consider the DBP
measured at the beginning of a clinical trial in a
subject as 92 mm Hg, denoted as R(t= 0), and DBP
measured at the end of 8 weeks of the trial,
55. Design dosage
regimen
To initiate drug therapy, the clinician must select
• Appropriate route of administration,
• Dosage and dosing interval.
Selection of a regimen depends on various patient and drug fa
ctors, including how rapidly therapeutic levels of a drug must be
achieved.
Therapy may consist of a single dose of a drug, for example, a
sleep-inducing agent, such as zolpidem.
56. Fixed-dose/fixed-
time regimens • Administration of a drug by
fixed doses rather than by
continuous infusion is often
more convenient.
• fixed doses of IV or oral
medications given at fixed
intervals result in time-
dependent fluctuations in the
circulating level of drug, which
contrasts with the smooth
ascent of drug concentration
with continuous infusion
57. Multiple IV Injections
Drug A in continues infusion
Drug B Twice daily injection
Drug C once daily injection