Bioavailability refers to the amount of drug that enters systemic circulation and is available at the site of action. It depends on the rate and extent of drug absorption from its dosage form. Many physiological and drug-specific factors can affect bioavailability such as pH, enzymes, blood flow, and food interactions. Careful evaluation and standardization of bioavailability is important for drug development and quality control to ensure accurate and safe dosing.
This presentation will give the students a basic knowledge about the pharmacokinetics of durgs. It will help them clear the basics before digging deep into the topic.
A Powerpoint presentation on drugs excretion and elimination suitable for UG medical students. This ppt is already presented to my students in one of the theory classes.
This presentation will give the students a basic knowledge about the pharmacokinetics of durgs. It will help them clear the basics before digging deep into the topic.
A Powerpoint presentation on drugs excretion and elimination suitable for UG medical students. This ppt is already presented to my students in one of the theory classes.
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
This presentation covers the nature and features of drug dependence. It also gives coverage to different psychological or biological models of drug addiction.
Drug Dependence & Abuse - Presentation by Akshay AnandAkshay Anand
A presentation on Drug Dependence and Drug Abuse that explains in brief about the various practices of substance abuse and dependence and the medicinal agents and drugs that can be used to overcome or treat such abuses. This was presented as a part of curriculum by Akshay Anand in Sree Siddaganga College of Pharmacy during May 2013.
“ Bioavailability-
means the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action."
Fundamental concept of modified drug releaseAbhinayJha3
Different Terminologies used in a modified release
1. Sustained release
2. Delayed release
3. Prolonged release
4. Extended-release
5. Controlled release
6. Site-specific targeting and receptor targeting
SELECTION OF DRUG CANDIDATE FOR ORAL SUSTAINED RELEASE SYSTEMS, BIOPHARMACEUTICAL CLASSIFICATION SYSTEM.
Fundamental concept of modified drug releaseAbhinayJha3
BIOPHARMACEUTICAL CLASSIFICATION SYSTEM
Different Terminologies used in a modified release
1. Sustained release
2. Delayed release
3. Prolonged release
4. Extended-release
5. Controlled release
6. Site-specific targeting and receptor targeting
Bioavailability is rate and extent of drug absorption
The relative amount of administered dose of drug that reaches to its site of action from the site and dose of administration in an unchanged form. The rate at which this phenomenon occurs is known as BIOAVAILABILITY
Here site of action refers to plasma or systemic circulation and unchanged form refers to therapeutically active form
Bioavailabile Dose:- Fraction of administered dose of drug which reaches to site of action is bioavailable dose.
CLINICAL SIGNIFICANCE OF BIOEQUIVALENCE STUDIES, BIOEQUIVALENCE, REASONS TO PERFORM BIOEQUIVALENCE STUDIES , NEED FOR BIOEQUIVALENCE STUDIES, IMPORTANCE OF BIOEQUIVALANCE STUDIES, DETERMINATION OF BIOEQUIVALENCE OF A DRUG PRODUCT, CLINICAL SIGNIFICANCE.
Drug-drug interactions(DDI) are one of the commonest causes of medication error, particularly in the elderly due to poly-therapy, with a prevalence of 20-40%. Drug interactions represent factors of uncertainty in many therapeutic situations. Drug–drug interactions can cause profound clinical effects, either by reducing therapeutic efficacy or enhancing toxicity of drugs. With an increasing frequency in polypharmacy, DDIs are one of the major causes for drug withdrawal from the market. In particular, poly-therapy increases the complexity of therapeutic management and thereby the risk of clinically important DDIs, which can both induce the development of adverse drug reactions or reduce the clinical efficacy. Although DDIs can result in alterations of either drug pharmacokinetics (PK), pharmacodynamics(PD), or both, it is the pharmacokinetic drug interactions that is clinically significant. PK drug interactions, typically characterized by alterations of plasma concentration–time profiles, could be attributed to changes in processes of absorption, distribution, metabolism, and excretion of a drug substance mediated by another drug when they are given concomitantly. In this review we mainly focused on the pharmacokinetic drug interactions with various drug examples and their mechanism of drug interactions that are clinically significant.
CHAPTER 1 SEMESTER V - ROLE OF PEADIATRIC NURSE.pdfSachin Sharma
Pediatric nurses play a vital role in the health and well-being of children. Their responsibilities are wide-ranging, and their objectives can be categorized into several key areas:
1. Direct Patient Care:
Objective: Provide comprehensive and compassionate care to infants, children, and adolescents in various healthcare settings (hospitals, clinics, etc.).
This includes tasks like:
Monitoring vital signs and physical condition.
Administering medications and treatments.
Performing procedures as directed by doctors.
Assisting with daily living activities (bathing, feeding).
Providing emotional support and pain management.
2. Health Promotion and Education:
Objective: Promote healthy behaviors and educate children, families, and communities about preventive healthcare.
This includes tasks like:
Administering vaccinations.
Providing education on nutrition, hygiene, and development.
Offering breastfeeding and childbirth support.
Counseling families on safety and injury prevention.
3. Collaboration and Advocacy:
Objective: Collaborate effectively with doctors, social workers, therapists, and other healthcare professionals to ensure coordinated care for children.
Objective: Advocate for the rights and best interests of their patients, especially when children cannot speak for themselves.
This includes tasks like:
Communicating effectively with healthcare teams.
Identifying and addressing potential risks to child welfare.
Educating families about their child's condition and treatment options.
4. Professional Development and Research:
Objective: Stay up-to-date on the latest advancements in pediatric healthcare through continuing education and research.
Objective: Contribute to improving the quality of care for children by participating in research initiatives.
This includes tasks like:
Attending workshops and conferences on pediatric nursing.
Participating in clinical trials related to child health.
Implementing evidence-based practices into their daily routines.
By fulfilling these objectives, pediatric nurses play a crucial role in ensuring the optimal health and well-being of children throughout all stages of their development.
Defecation
Normal defecation begins with movement in the left colon, moving stool toward the anus. When stool reaches the rectum, the distention causes relaxation of the internal sphincter and an awareness of the need to defecate. At the time of defecation, the external sphincter relaxes, and abdominal muscles contract, increasing intrarectal pressure and forcing the stool out
The Valsalva maneuver exerts pressure to expel faeces through a voluntary contraction of the abdominal muscles while maintaining forced expiration against a closed airway. Patients with cardiovascular disease, glaucoma, increased intracranial pressure, or a new surgical wound are at greater risk for cardiac dysrhythmias and elevated blood pressure with the Valsalva maneuver and need to avoid straining to pass the stool.
Normal defecation is painless, resulting in passage of soft, formed stool
CONSTIPATION
Constipation is a symptom, not a disease. Improper diet, reduced fluid intake, lack of exercise, and certain medications can cause constipation. For example, patients receiving opiates for pain after surgery often require a stool softener or laxative to prevent constipation. The signs of constipation include infrequent bowel movements (less than every 3 days), difficulty passing stools, excessive straining, inability to defecate at will, and hard feaces
IMPACTION
Fecal impaction results from unrelieved constipation. It is a collection of hardened feces wedged in the rectum that a person cannot expel. In cases of severe impaction the mass extends up into the sigmoid colon.
DIARRHEA
Diarrhea is an increase in the number of stools and the passage of liquid, unformed feces. It is associated with disorders affecting digestion, absorption, and secretion in the GI tract. Intestinal contents pass through the small and large intestine too quickly to allow for the usual absorption of fluid and nutrients. Irritation within the colon results in increased mucus secretion. As a result, feces become watery, and the patient is unable to control the urge to defecate. Normally an anal bag is safe and effective in long-term treatment of patients with fecal incontinence at home, in hospice, or in the hospital. Fecal incontinence is expensive and a potentially dangerous condition in terms of contamination and risk of skin ulceration
HEMORRHOIDS
Hemorrhoids are dilated, engorged veins in the lining of the rectum. They are either external or internal.
FLATULENCE
As gas accumulates in the lumen of the intestines, the bowel wall stretches and distends (flatulence). It is a common cause of abdominal fullness, pain, and cramping. Normally intestinal gas escapes through the mouth (belching) or the anus (passing of flatus)
FECAL INCONTINENCE
Fecal incontinence is the inability to control passage of feces and gas from the anus. Incontinence harms a patient’s body image
PREPARATION AND GIVING OF LAXATIVESACCORDING TO POTTER AND PERRY,
An enema is the instillation of a solution into the rectum and sig
The dimensions of healthcare quality refer to various attributes or aspects that define the standard of healthcare services. These dimensions are used to evaluate, measure, and improve the quality of care provided to patients. A comprehensive understanding of these dimensions ensures that healthcare systems can address various aspects of patient care effectively and holistically. Dimensions of Healthcare Quality and Performance of care include the following; Appropriateness, Availability, Competence, Continuity, Effectiveness, Efficiency, Efficacy, Prevention, Respect and Care, Safety as well as Timeliness.
Struggling with intense fears that disrupt your life? At Renew Life Hypnosis, we offer specialized hypnosis to overcome fear. Phobias are exaggerated fears, often stemming from past traumas or learned behaviors. Hypnotherapy addresses these deep-seated fears by accessing the subconscious mind, helping you change your reactions to phobic triggers. Our expert therapists guide you into a state of deep relaxation, allowing you to transform your responses and reduce anxiety. Experience increased confidence and freedom from phobias with our personalized approach. Ready to live a fear-free life? Visit us at Renew Life Hypnosis..
CRISPR-Cas9, a revolutionary gene-editing tool, holds immense potential to reshape medicine, agriculture, and our understanding of life. But like any powerful tool, it comes with ethical considerations.
Unveiling CRISPR: This naturally occurring bacterial defense system (crRNA & Cas9 protein) fights viruses. Scientists repurposed it for precise gene editing (correction, deletion, insertion) by targeting specific DNA sequences.
The Promise: CRISPR offers exciting possibilities:
Gene Therapy: Correcting genetic diseases like cystic fibrosis.
Agriculture: Engineering crops resistant to pests and harsh environments.
Research: Studying gene function to unlock new knowledge.
The Peril: Ethical concerns demand attention:
Off-target Effects: Unintended DNA edits can have unforeseen consequences.
Eugenics: Misusing CRISPR for designer babies raises social and ethical questions.
Equity: High costs could limit access to this potentially life-saving technology.
The Path Forward: Responsible development is crucial:
International Collaboration: Clear guidelines are needed for research and human trials.
Public Education: Open discussions ensure informed decisions about CRISPR.
Prioritize Safety and Ethics: Safety and ethical principles must be paramount.
CRISPR offers a powerful tool for a better future, but responsible development and addressing ethical concerns are essential. By prioritizing safety, fostering open dialogue, and ensuring equitable access, we can harness CRISPR's power for the benefit of all. (2998 characters)
QA Paediatric dentistry department, Hospital Melaka 2020Azreen Aj
QA study - To improve the 6th monthly recall rate post-comprehensive dental treatment under general anaesthesia in paediatric dentistry department, Hospital Melaka
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Lectures 11 Bioavailability
1. Bio availability
Its clinical significance &
Factors affecting bioavailability
Dr. Ghulam Saqulain
M.B.B.S., D.L.O., F.C.P.S
Head of Department of ENT
Capital Hospital, Islamabad
2. Bio availability
“Bioavailability is a measurement
of the extent of a therapeutically active medicine that reaches
the systemic circulation and is therefore available at the site
of action”.
2
3. The therapeutic effectiveness of a drug depends
upon the ability of the dosage form to deliver the
medication to its site of action at a rate & amount
sufficient to elicit the desired Pharmacological
response.
This attribute of the dosage form is referred to as
physiologic availability or bioavailability.
4. Bioavailability example:-
A hypothetical drug given orally has a
bioavailability of 50%
(or 0.5), this is due to:
1. incomplete absorption in the GI tract so that
only 70% of the initial dose is absorbed.
2. subsequent metabolism of a further 20% before
it reaches the systemic circulation (e.g. first pass
through the liver).
Therefore only 50% of the original oral dose
reaches the systemic circulation.
6. The influence of route of administration on drug’s
bioavailability is generally in the following order:
parenteral > oral > rectal > topical
Most drugs are administered orally, for reason of stability and
convenience.
6
8. Objectives of bioavailability studies
It is important in:
1. Primary stages of development of a suitable
dosage form
2. Determination of influence of excipients, patient
related factors and interaction with other drugs on
the efficiency of absorption.
8
9. 3. Development of new formulations of the existing
drugs.
4. Control of quality of a drug product during early
stages of marketing (to determine the influence of
processing factors, storage & stability of
absorption).
9
10. Considerations in bioavailability studies
Bioavailability – absolute / relative
Single dose / multiple dose
Human volunteer – healthy subject / patients
10
11. Absolute vs. Relative
Absolute bioavailability : when the systemic
availability of the drug administered orally is
determined in comparison to its i.v. administration.
Relative bioavailability : when the systemic
availability of the drug administered orally is
compared with that of an oral standard of the same
drug.
11
12. Plasma concentration vs. time profile of a drug ingested
orally & intravenously.
0
10
20
30
40
50
60
70
0 2 4 6 8 10
Plasma
concentration
Time (hours)
i.v. route
oral route
12
13. Single dose vs. multiple dose
Single dose
Very common & easy
Less exposure to drug &
less tedious
Difficult to predict
steady state
Multiple dose
Difficult to control
More exposure to drug
& tedious
Time consuming
13
15. Multiple dose study has several advantages like:
1. More accurately reflects the manner in which the drug
should be used.
2. Drugs levels are higher due to cumulative effect which
makes its determination possible even by less sensitive
analytical methods.
15
Single dose vs. multiple dose
16. 3. Better evaluation of the performance of controlled
release formulation is possible.
4. Small intersubject variability is observed which
allows use of fewer subjects.
5. Nonlinearity in pharmacokinetics, if present, can be
easily detected.
16
17. Human volunteer – healthy subject vs. patients
Ideally, the bioavailability study should be carried
out in patients for whom the drug is intended to be
used.
Advantages :
1. Patient is benefited from the study.
2. Reflects better therapeutic efficacy of drug.
17
18. 3. Drug absorption pattern in disease state can be
evaluated.
4. Avoids the ethical quandary of administering drug
to healthy subjects.
18
19. There are some drawbacks of using patients as
volunteers.
Stringent conditions such as fasting state required is
difficult to be followed by the patients.
Studies are therefore performed in young (20-40
yrs.), healthy males adult volunteers.
19
20. Female volunteers are used only when drugs such as
oral contraceptives are to be tested.
They must be informed about the importance of:
Study
conditions to be followed
Possible hazards if any.
20
21. Medical examination should be performed.
Drug washout period for min. of ten biological half
lives must be allowed for between two studies in
same subject.
21
23. Plasma level time studies or The plasma concentration – time
curve or blood level curve.
A direct relationship exists b/w concentration of drug at the
site of action & concentration of drug in the plasma.
Serial blood samples are taken after drug administration &
analyzed for drug concentration.
A typical blood level curve obtained after oral administration of
drug.
23
Blood Analysis:
25. Acute pharmacological response
Bioavailability can be determined from the acute
pharmacologic effect – time curve
DISADVANTAGE is that pharmacological response tends to more
variable & accurate correlation between the measured response &
drug available from the formulation is difficult.
25
26. Therapeutic response
This method is based on the observing the clinical response to a
drug formulation given to a patients suffering from disease for
which it is intended to be used.
Ex …for anti inflammatory drugs, the reduction in the inflammation
is determined.
The major DRAWBACK is …quantification of observed response
is too improper to allow for reasonable assessment of relative
bioavailability between two dosage forms of a same drug.
26
28. Clinical importance of bioequivalence studies
Bioequivalence of different formulations of the same drug
substance involves equivalence with respect to the rate and
extent of systemic absorption.
Generally two formulations whose rate and extent of
absorption differ by 20% or less are considered bioequivalent
28
29. When a therapeutic objectives of the drug are considered, an
equivalent clinical response should be obtained from the
comparison dosage form if the plasma drug concentration
remain above MEC for appropriate interval and don’t reach
the MTC.
30. Bioequivalence studies should be conducted for the
comparison of two medicinal products containing the same
active substance.
Two products marketed by different licensees, containing
same active ingredient(s), must be shown to be
therapeutically equivalent to one another in order to be
considered interchangeable.
30
31. Clinical Significance
Change in Bioavailability may lead to under/ over
medication
Under Medication – Therapeutic failure
Hazardous specially for drugs like Antimicrobials, anticonvulsants
and oral antidiabetic agents
Over medication – Toxicity
32. Indiscriminate change of preparation from other
companies must be avoided. (change of drug brand
may lead to Non-bioequivalence)
Use of Alternate routes:
Drugs with high hepatic first pass metabolism should be
given by routes other than oral. ie., sublingual,
transdermal eg., Nitroglycerine
33. High oral doses: Some drugs have high hepatic
extraction ratio.
Less dose in hepatic Disease: In severe hepatic
cirrhosis/ portal systemic shunts, the dose of the
drugs with large extraction ration and hepatic first
pass effect should be reduced otherwise toxicity
34. Physiologic factors
1. pH Stomach ~ 1 and intestine ~ 6
2. Surface area of the of the intestine – microvilli
3. Presence of carrier proteins for absorption
4. Enzymes: endogenous and bacterial
5. GI blood flow
6. Gastric Emptying & intestinal transit
Factors Affecting Bioavailability
35. Physicochemical Properties of the Drug
Water & lipid solubility
Molecular size
Stability in GI environment (pH)
Specificity for carrier proteins and enzymes
36. Food & Drug
Food can affect both rate and extent of absorption.
Effect depends on the drug
and the nature of the meal.
Food can increase / decrease or have no effect on either rate or
extent
FOOD Affects pH, Blood flow, Gastric emptying & Interactions with
enzymes
DRUGS Affect Blood flow, Gastric emptying & Interactions with
enzymes