1) Pharmacokinetics involves the processes of absorption, distribution, metabolism, and excretion that determine the concentration of drugs in the body over time.
2) Absorption refers to how drugs enter the bloodstream after administration by various routes like oral, parenteral, topical. Factors like dosage form, food, and pH affect absorption.
3) Distribution describes how drugs are transported in blood and delivered to tissues throughout the body, influenced by properties like protein binding and water/fat solubility.
4) Metabolism (biotransformation) alters drugs chemically in the liver mainly, producing inactive or active metabolites. The first-pass effect impacts oral bioavailability.
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 is the second part of my presentation. It is all about the review on Routes and rights of drug administration. The slide also covers IP & Drug Laws too.
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 is the second part of my presentation. It is all about the review on Routes and rights of drug administration. The slide also covers IP & Drug Laws too.
Drugs may be administered by various routes. The choice of the route in a given patient depends on the tissue or organ to be treated, the characteristics of the drug and urgency of the situation, etc. Knowledge of the advantages and disadvantages of the different routes of administration is essential. The routes can be broadly divided into Enteral, Parenteral, and Local.
INTRODUCTION OF ABSORPTION
TRANSPORT PROCESS
FACTORS AFFECTING DRUG ABSORPTION WITH EXAMPLES:
1) Physiological factors
2) physiochemical factors
3) pharmaceutical factors
A brief presentation about the transport of drugs across the cell membrane including the many mechanisms and various transporters and a brief overview of the ABC and SLC superfamily of transporters.
Dosage forms and routes of drug administrationFatenAlsadek
this presentation give an over review about Routes of drug administrations and dosage forms
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
In a broad sense, the pharmacology deals with the study of drugs and their interactions with living systems. This study includes sources, chemical properties, dose, biological effects, therapeutic uses, and adverse effects of drugs. i.e. Pharmacology is the study of how drugs act on biological systems and how the body responds to the drug.
It comprises all aspects of knowledge about drugs, but most importantly those that are relevant to effective and safe use for medicinal purposes. Pharmacology integrates the knowledge of many disciplines, including medicine, pharmacy, dentistry, nursing, and veterinary medicine. This integrative nature allows pharmacology to make unique and significant contributions to human health.
Pharmacology is crucial for:
discovering new medicines to help fight diseases
improving the effectiveness of medicines
reducing unwanted side effects of medicines
understanding why individuals differ in the way they respond to certain drugs, and why some others cause addiction
Drugs may be administered by various routes. The choice of the route in a given patient depends on the tissue or organ to be treated, the characteristics of the drug and urgency of the situation, etc. Knowledge of the advantages and disadvantages of the different routes of administration is essential. The routes can be broadly divided into Enteral, Parenteral, and Local.
INTRODUCTION OF ABSORPTION
TRANSPORT PROCESS
FACTORS AFFECTING DRUG ABSORPTION WITH EXAMPLES:
1) Physiological factors
2) physiochemical factors
3) pharmaceutical factors
A brief presentation about the transport of drugs across the cell membrane including the many mechanisms and various transporters and a brief overview of the ABC and SLC superfamily of transporters.
Dosage forms and routes of drug administrationFatenAlsadek
this presentation give an over review about Routes of drug administrations and dosage forms
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
In a broad sense, the pharmacology deals with the study of drugs and their interactions with living systems. This study includes sources, chemical properties, dose, biological effects, therapeutic uses, and adverse effects of drugs. i.e. Pharmacology is the study of how drugs act on biological systems and how the body responds to the drug.
It comprises all aspects of knowledge about drugs, but most importantly those that are relevant to effective and safe use for medicinal purposes. Pharmacology integrates the knowledge of many disciplines, including medicine, pharmacy, dentistry, nursing, and veterinary medicine. This integrative nature allows pharmacology to make unique and significant contributions to human health.
Pharmacology is crucial for:
discovering new medicines to help fight diseases
improving the effectiveness of medicines
reducing unwanted side effects of medicines
understanding why individuals differ in the way they respond to certain drugs, and why some others cause addiction
- Routes of administration
- First pass metabolism, bioavailablilty, drug distribution,
- Drug interactions with proteins, Drug metabolism, elimination, Half-life
General pharmacology Diploma in pharmacy second year YogeshShelake
The General pharmacology ,Toxicology & Pharmacotherapeutics
To Undastanding the general pharmacology & Definitions of PHARMACODYNAMECIS ,PHARMACOKINITICS (Absorbation,Distribution,Metabolism,Excreation )Pharmacology ,Toxicology ,Pharmacotherapeutic ,
Advantages of Routs of Administration & Their Disadvantages
Factors affecting of absorpation ,excreation of drug,factor modifing deug action
Pharmacokinetics (PK) is the study of how the body interacts with administered substances for the entire duration of exposure (medications for the sake of this article). This is closely related to but distinctly different from pharmacodynamics, which examines the drug's effect on the body more closely.
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
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
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.
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
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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2. Pharmacologic Principles
• Drug
Any chemical that affects the physiologic processes of a
living organism
• Pharmacology
The study or science of drugs
3. • Therapeutic ratio
– is the number indicating the ratio between lethal or toxic dose
and effective dose.
• Critical concentration
– Amount of drug that is needed to cause therapeutic effect
– Must be maintained in order for the drug to produce the desired
therapeutic effect in the body.
4. • Loading dose
– The starting dose that is higher than the dose usually used for tx
– Given so that the time for a drug to reach its critical conc will be hasten
• Dynamic equilibrium
– Result when drug reaches in the body and actual conc of the drug is
achieved involving the process of absorption, distribution, metabolism
and excretion
5. Pharmacologic Principles
• Knowledge of pharmacologic principles:
» why a drug is ordered
» how to administer drugs
» assessment of therapeutic benefits
» how to deal with toxic adverse effects
• The nurse with a sound knowledge base in pharmacology is better
equipped to implement the nursing process
7. Pharmacologic Principles
1) Pharmaceutics
The study of various drug forms
Deals with the delivery system
IV, PO, IM
Injection, capsule, timed-release, topical
Determines the rate at which the drug will dissolve and be absorbed
8. Pharmacologic Principles
1) Pharmaceutics
• The pharmaceutical phase is
concerned with the disintegration of the
dosage form or dissolution of the drug
in the body
• How the dosage forms affect the way
the body metabolizes the drug and how
the drug affects the body
9. Pharmacologic Principles
1) Pharmaceutics
The dosage form determines the rate at which a drug
enters the body
A variety of dosage forms are available to increase the
accuracy of dosing and to obtain therapeutic
responses with the least amount of adverse effects
11. Pharmacologic Principles
2) Pharmacokinetics
– The study of what actually happens to a drug from the time it enters the body until it
has left the body
a. Absorption
movement of a drug from the site of administration
b. Distribution
transport of a drug in the bloodstream
c. Metabolism
alteration of a drug in the body
d. Excretion
elimination of the drug or its compound from the body
12. 2) Pharmacokinetics
a. Absorption
• What happens to a drug from the time it is introduced to the body until it
reaches the circulating fluids and tissues.
Areas in the body where drug can be absorbed
• GI tract either oral/rectal
• Mucous membranes
• Skin
• Lungs
• Muscle
• Subcutaneous tissues
13. 2) Pharmacokinetics
a. Absorption
• The route of administration affects the rate and extent of absorption of that
drug
A. Enteral (GI tract)
B. Parenteral
C. Topical
• The extent of absorption is called BIOAVAILABILITY
– portion of the drug that reaches the systemic circulation
KEY POINT: not all drug formulations are equally absorbed
14. Oral Drugs
• Dosage
– determined by how much of the drug is
required to be taken by mouth to reach
desired effect.
15. Mechanism of Drug Absorption
• Passive Diffusion
– movement of a drug from higher to lower concentration.
• Carrier Mediated Absorption(Facilitated diffusion)
– no cellular energy. Drug molecules combine with a carrier substance such as
enzyme or other protein.
• Active Transport
– drug molecules move from an area of low concentration to an area of high
concentration; transported by the carrier molecules as cellular energy.
• Pinocytosis
– occurs when a cell engulfs drug particles and moves them across the cell
membrane and into the inner cell.
16. a. Absorption of oral drugs
Factors that affect absorption
varies according to the dosage form and route
1. Food or fluids administered with the drug
– help or hinder absorption
– food may delay transit to the intestines
– high fat foods may help some fat soluble drugs
2. Dosage formulation
– determined by how much of the drug is required to be taken by mouth to given the
desired affect.
– tablets, capsules- some dissolve in the stomach, others in the intestine.
– Certain types are coated to dissolve slowly and have timed release.
– Some types are formulated with small particles that dissolve super fast- ie: micronized
glyburide
20. a. Absorption of oral drugs
Factors that affect absorption
varies according to the dosage form and route
3. Status of the absorptive surface
– portions of the small intestine may be missing or damaged
4. Rate of blood flow to the small intestine
– blood flow may be decrease to the intestine in certain instances
– i.e. sepsis, exercise, labor
5. Acidity of the stomach
– food increases gastric acid production leading to decreased stomach pH. Drugs are formulated to dissolve at a specific pH
level.
6. Status of GI motility
– Fast or slow transit time due to pathology, conditions, or other medications change transit time
21. a. Absorption of oral drugs
Some drugs need to be taken on an empty stomach
with a full glass of water
Other drugs should be taken on a full stomach or
with food to enhance absorption or minimize gastric
irritation
22. • + food in stomach
– usually decreases absorption of drugs, but it may increase absorption for a few
specific medications.
• pH of the stomach
– Alkaline drugs are absorbed more readily in an alkaline environment
– acid drugs are absorbed more readily in an acid environment.
• form of the drug
– liquid drugs being absorbed the fastest and enteric-coated tablets the slowest.
23. a. Absorption of oral drugs
Drugs are absorbed into the mesenteric blood system and go to the liver for
biotransformation before traveling on to the general systemic circulation.
This is called the
FIRST PASS EFFECT
• Therefore some of the drug is inactivated and not all will be available for use
at its intended site of action.
• Drugs are formulated to account for this difference in availability to the
tissues- called (bioavailability)
• This is why different forms of drugs are not equal
24. First-Pass Effect
The metabolism of a drug and its passage from the
liver into the circulation.
• oral route may be extensively metabolized by the liver before
reaching the systemic circulation (high first-pass effect).
• The same drug—given IV—bypasses the liver, preventing the
first-pass effect from taking place, and more drug reaches the
circulation.
25. First-Pass Effect
• Routes that bypass the liver:
– Sublingual Transdermal
– Buccal Vaginal
– Rectal* Intramuscular
– Intravenous Subcutaneous
– Intranasal Inhalation
*Rectal route undergoes a higher degree of first-pass effects than the other
routes listed.
26. What else might influence oral drug
absorption?
• Food in stomach
• Certain juices – grapefruit juice
• Milk – binds with molecules of some drugs so that the drug is never
absorbed
• Orange juice – enhances absorption of iron taken orally
• The coating on the tablet: chewable, enteric coated (breakdown
occurs in small intestine), slow release capsules
27. a. Absorption of parenteral
drugs
Parental drugs have no first pass effect
• Intravenous
– rapid and 100% bioavailable
– Avoids problems with stomach acid and intestinal absorption issues
• Intramuscular
– not as rapid as IV- will absorb better if there is a good blood supply
• Some IM medications are in DEPOT form- have a very slow absorption time (even
months)- due to the formulation
– these drugs should not be given IV- can cause an embolus
28. a. Absorption of parenteral
drugs
Parenteral Route
• Intravenous*
• Intramuscular
• Subcutaneous
• Intradermal
• Intrathecal
• Intraarticular
*Fastest delivery into the blood circulation
29. a. Absorption of topical drugs
• Many different formulations of topical drugs
• May be given for local or systemic effect
30. a. Absorption of topical drugs
Topical Route
• Skin (including transdermal patches)
• Eyes
• Ears
• Nose
• Lungs (inhalation)
• Vagina
31. a. Absorption of oral drugs
sublingual and buccal
Avoids the first pass effect
• Absorbed into the highly vascularized tissue under the tongue or between
the cheek and the gum- the oral mucosa
• Bypass the liver
• Rapidly absorbed
32. a. Absorption
• The ROUTE of administration affects
the rate and extent of absorption
of that drug
33. 2) Pharmacokinetics
The transport of a drug in the body by the
bloodstream to its site of action
a. Absorption
b. Distribution
c. Metabolism
d. Excretion
34. b. Distribution
• Drugs are distributed first to areas that have extensive blood
supplies
heart liver kidneys brain
• Areas of slower distribution are
muscles skin fat
• Sites like bone and brain may be very difficult for drugs to reach due
to either poor blood supply or barriers
35. b. Distribution of drugs
Factors that affect distribution
1. Protein-binding
• Many drugs bind to proteins in the bloodstream
-Albumin is the main protein to bind with drugs
-Drugs bound to proteins are not available for use in other tissues & organs called protein bound
-Drugs not bound to protein are available to act at
the intended site of action and exert their effects
*called free drug
• Drug companies adjust drug dosages to allow for protein binding
36. b. Distribution of drugs
Factors that affect distribution
• If a patient has low albumin more free drug is available and the
patient may have increased adverse effects (toxicity)
• If 2 drugs are given that are highly protein bound they compete for
binding sites on the albumin.
– The drugs will have higher levels of ―free‖ drug and the patient may have
increased adverse effects
• This fact is significant because only the unbound or free drug is able
to reach the target tissue and exert its pharmacologic effect.
37. b. Distribution of drugs
Factors that affect distribution
2. Water soluble vs fat soluble
• Water soluble drugs
– tend to stay in the bloodstream and have slow absorption into the tissues.
• Fat soluble drugs
– are distributed to the tissues more quickly
– the more lipid soluble the drug is, the higher its ability to reach all cells in the body.
38. b. Distribution of drugs
Factors that affect distribution
3. Blood Flow
a. Blood-brain barrier
– network of capillaries that makes it more difficult for drugs to pass through--will
allow some fat soluble drugs to pass through
– Brain capillary endothelium have special characteristics that limit the passage of
drugs
b. Placental barrier
– in general whatever mom gets the fetus gets
39. b. Distribution of drugs
Factors that affect distribution
4. Blood Flow
– If drug is circulating in the bloodstream, it will gain greater access to tissues that
are highly perfused.
– Therefore, if the blood circulation is poor, the result is insufficient drug
distribution.
5. Binding to sub-cellular components
– There are drugs that are bound within specific cells in which they are causing
their effect and are unable to leave the cell to be carried in the blood stream.
40. 2) Pharmacokinetics
a. Absorption
b. Distribution
c. Metabolism
d. Excretion
41. c. Metabolism of drugs
• Also Known as Biotransformation
• Drugs are changed into new, less active chemicals
• It takes place mainly in the liver and produces
1. An inactive metabolite
2. A more soluble compound
3. A more potent metabolite
42. c. Metabolism
(biotransformation)
Organs or body tissues responsible for
metabolism:
– Liver (mainly)
– Skeletal muscle
– Kidneys
– Lungs
– Plasma
– Intestinal mucosa
43. c. Metabolism (biotransformation)
Hepatic Cytochrome P-450 enzyme system
• These enzymes control a variety of biochemical reactions that aid in
metabolism
• These enzymes are largely targeted against lipid-soluble and
nonpolar (no charge) drugs which are difficult to eliminate
• These include the majority of medications
44. c. Metabolism (biotransformation)
The capability of the liver to metabolize drugs varies widely between patients
• Age
Elderly have decreased hepatic enzymes
Neonates have immature liver functions
• Genetics
certain genetic groups metabolize drugs at
different rates
• Foods
Grapefruit and certain other foods
• Concurrent use of other medications
Tylenol and many other drugs
• Diseases
Cardiovascular or Renal dysfunction
45. c. Metabolism
(biotransformation)
Factors that decrease (delay) metabolism
• Cardiovascular dysfunction
• Renal insufficiency
• Starvation
• Obstructive jaundice
• Slow acetylator (metabolism of drug)
• Erythromycin or ketoconazole drug therapy
46. c. Metabolism
(biotransformation)
Decreased drug metabolism
results in:
• Accumulation of drugs
• Prolonged action of the drugs
• Possible toxic levels
47. c. Metabolism
(biotransformation)
Factors that increase (stimulate) metabolism
• Fast acetylator
• Drugs that stimulate the formation of new enzymes
Barbiturate therapy
Rifampin therapy
49. c. Metabolism (biotransformation)
FIRST PASS EFFECT
• The initial metabolism of a drug and its passage from the liver into the
circulation
– A drug given via the oral route may be extensively metabolized (inactivated or
changed) by the liver before reaching the systemic circulation high first-pass effect
• Oral drugs ( because they go through the liver) may not be 100% available
to reach the intended sites of action
50. c. Metabolism (biotransformation)
FIRST PASS EFFECT– routes of administration
• The same drug—given IV—initially bypasses the liver, getting to it’s
intended site of action more quickly and preventing the first-pass effect
from taking place.
• IV drugs are 100% available to the body (bioavailability)
Cefuroxime:
IV = 750mg/ml
oral = 500 mg/ml
51. c. Metabolism (biotransformation)
FIRST PASS EFFECT– routes of administration
• The first-pass effect is one reason why drug dosages and frequency
of administration are different depending on the route of
administration
IV DOSE is not always equal to an ORAL DOSE
52. 2) Pharmacokinetics
a. Absorption
b. Distribution
c. Metabolism
d. Excretion
53. d. Excretion
The elimination of drugs from the body
• Kidneys (main organ)
Whether the drug is an original compound
(parent compound), an active or an inactive
metabolite----
• Liver
• Bowel
– Biliary excretion
– Enterohepatic recirculation
54. d. Excretion
The kidneys remove the drugs that are unbound
(free) in the plasma
Certain drugs (like highly protein bound drugs)
can’t be excreted and are reabsorbed back into
the system
55. d. Excretion
• Patients with renal failure will not be able to
excrete drugs efficiently
• Drug levels will increase
• Patients may experience more adverse effects
and toxicity
56. Pharmacokinetics
Onset, Peak, Duration and Trough
Onset
• The time it takes for the drug to elicit a therapeutic
response
INSULIN ONSET PEAK DURATION
Ultra rapid acting 15 mins. 2-4 hrs. 6-8 hrs.
Insulin analog
(Humalog)
57. Pharmacokinetics
Onset, Peak, Duration and Trough
Peak
• The time it takes for a drug to reach its maximum therapeutic
response
• Oral = 1-3hrs
• IV = 10mins
• good time for a dressing change or other painful procedure
• Good time to draw blood
INSULIN ONSET PEAK DURATION
Ultra rapid acting 15 mins. 2-4 hrs. 6-8 hrs.
Insulin analog
(Humalog)
58. Pharmacokinetics
Onset, Peak, Duration and Trough
Duration
• The time a drug concentration is sufficient to elicit a therapeutic
response
how long is it going to last- (anticipate the next dose)
INSULIN ONSET PEAK DURATION
Ultra rapid acting 15 mins. 2-4 hrs. 6-8 hrs.
Insulin analog
(Humalog)
59. Pharmacokinetics
Onset, Peak, Duration and Trough
Trough
• Lowest blood level of a drug
Note:
If either the peak or trough levels is too high, toxicity can occur.
If the peak is too low, no therapeutic effect is achieved.
61. Laboratory Values
• Laboratory values reflecting function of liver and kidneys need to be
looked at:
– BUN and Creatinine – kidney function
– LFT or liver function tests:
• ALT – alanine aminotransferase (elevated in hepatitis)
• AST or SGOT– aspartate aminotransferase – elevated in liver disease
• ALP – elevated in biliary tract disease
• Bilirubin levels – infants – gallstones in adults
62. Serum Drug Levels
• Laboratory measurement of the amount of drug
in the blood at a particular time
• A minimum effective concentration (MEC) must
be present before a drug exerts its action on a
cell.
63. Toxic Levels
• Excessive level of a drug in the body
– Single large dose
– Repeated small doses
– Slow metabolism which allows drug to accumulate in
the body
– Slow excretion from the body by the kidneys or
gastrointestinal tract
64. Yes, laboratory values are
important!
• Serum drug levels indicate the onset, peak
and duration of the drug action
65. Do we do serum drug levels for all
drugs?
• No
• When do we need them?
– Drugs with narrow margin of safety (digoxin, aminoglycoside
antibiotics, lithium)
– To check to see if the drug is at therapeutic levels – seizure
medications
– When drug overdose is suspected
67. Pharmacokinetics
• Half-life
• The time it takes for one half of the original amount of a drug in the
body to be removed
• A measure of the rate at which drugs are removed from the body
• Most drugs are considered to be effectively removed after about five
half-lives**
68. Why is this important?
• Half-life determines how often a drug is given
– Daily in the morning
– At bedtime
– Q.I.D - four times a day
– T.I.D – three times a day
– Q4 hours – every four hours
– Q 12 hours – 9 am and 9 pm
69. Pharmacokinetics
Short ½ life– need to take frequently
compliance may be a problem
example: acyclovir 5 times daily
Long ½ life- pt has an adverse reaction
the drug will be in the body for
hours or days
example: Cialis T1/2 = 17 hours
(Viagra might have been a better choice for this pt with a T1/2 of 4 hours)
70. Pharmacokinetics
• Steady state
• Where the amount of drug excreted is equal to the amount of drug absorbed
with each dose
• Giving more drug could cause toxicity
• Giving less drug would not be therapeutic
• Typically occurs after 4-5 half-lives of administration
71. Pharmacokinetics
Steady state
• Drugs with a very long half-life make take a longer time to reach a steady
state
- some antidepressants
• With certain drugs, to reach a steady state more quickly, a LOADING
DOSE may be ordered
This is a higher initial dose