Assignment 2

Submitted by:
Name:
Syeda Zoha Fatima
Roll Number:
Fa22-MSPY-025
Submitted to:
Teacher Name:
Ma’am Amnah
Course:
Physophysiology and Psychopharmacology
Department of Psychology
 Principles of Psychopharmacology
 Pharmacokinetics
 Pharmacodynamics
Pharmacokinetics
The term “Pharmacokinetics” is derived from Greek words Pharmakon (drug) and Kinesis
(movement). It is the quantitative study of drug movement in, through and out of the body and
their relationship with the pharmacological, therapeutic or toxicological response in man or
animals
The mathematical analysis of the time courses of the processes of adsorption, distribution,
metabolism and excretion of a drug administered to a subject, Pharmacokinetics describes the
relationship between drug levels in various regions ('compartments') of the body and time.
From the moment that a drug enters the body, the body recognizes it and processes it in a unique
way, according to the individual characteristics of the drug. This information can be used to
improve the administration and use of medicines.
Principles of Pharmacokinetics:

 Absorption: Describes how the drug moves from the site of administration to the site
of action.
 Distribution: Describes the journey of the drug through the bloodstream to various
tissues of the body.
 Metabolism: Describes the process that breaks down the drug.
 Excretion: Describes the removal of the drug from the body.
 1) Absorption: Absorption is the movement of a drug from its site of administration to the
bloodstream. The rate and extent of drug absorption depend on multiple factors, such
as:
 Route of administration
 The formulation and chemical properties of a drug
 Drug-food interactions
2) Distribution: Distribution is the process by which drug passes from the bloodstream to
body tissues and organs. It is how a drug moves from intravascular space, e.g. blood
vessels, to extravascular space, e.g. body tissues, as it is carried around the body by the
circulatory system factors that affect distribution include:
 Solubility, including pKa values
 Effect of pH on solubility;
 Partition/distribution coefficients
3) Metabolism: Metabolism describes the chemical reactions that change drugs into
compounds which are easier to eliminate. The products of these chemical reactions are
called metabolites. The reactions are catalysed by enzymes and happen mostly in the
liver, though some changes take place in the gut wall, lungs and blood plasma. In these
reactions non-polar drug molecules are chemically changed into more polar molecules.
Compounds consisting of non-polar molecules tend to be soluble in fats and insoluble in water.
polar molecules tend to be insoluble in fats and soluble in water.

Metabolism is often divided into two phases:

a) Phase 1 metabolism involves chemical reactions such as oxidation (most common),

reduction and hydrolysis. There are three possible results of phase 1 metabolism. The
drug becomes completely inactive. In other words, the metabolites are pharmacologically
inactive. One or more of the metabolites are pharmacologically active, but less so than
 the original drug. The original substance is not pharmacologically active, but one of its
metabolites is. The original substance is called a prodrug

Warfarin is used as an anti-coagulant. None of its metabolites are pharmacologically active and they are
excreted by kidney.

b) Phase 2 metabolism involves reactions that chemically change the drug or phase 1 metabolites
into compounds that are soluble enough to be excreted in urine. In these reactions, the
molecule drug or metabolite) is attached to an ionisable grouping. This is called conjugation and
the product is called a conjugate. Metabolites formed in phase 2 are unlikely to be
pharmacologically active.
4) Exceretion: the process of removing a drug and its metabolites from the body. This usually
happens in the kidneys via urine produced in them. Other possible routes include bile,
saliva, sweat, tears and faeces. Most drugs are insufficiently polar (and, therefore, water
soluble) to be excreted directly.

Routes of Drug Administration:

The route of administration is determined primarily by the properties of the drug (for example,
water or lipid solubility, ionization) and by the their apeutic objectives (for example, the
desirability of a rapid onset of action, the need for long-term treatment, or restriction of delivery
to a local site). Major routes of drug administration include enteral, parenteral, and topi- cal
among others.
1) Enteral: Administering a drug by mouth, is the safest and most common, convenient, and
economical method of drug administration. it may be swallowed, or placed under the tongue.

a) Oral: This is convenient and is indicated for patients who can ingest and tolerate an oral form
of medication. giving a drug by mouth provides many advantages to the patient. Oral drugs are
easily self-administered and, compared to drugs given parenterally. Advantages are: The oral
route is the most common route for drug administration. It is the most preferred route, due to its
advantages, such as non-invasiveness, patient compliance and convenience of drug
administration. Disadvantages: Although solid-dose forms such as tablets and capsules have a
high degree of drug stability and provide accurate dosage, the oral route is problematic because
of the unpredictable nature of gastrointestinal absorption.
Example: Benzodiazepines, Hallucinogens, MDMA.

(i) Enteric coated: Enteric coating is a polymer applied to oral medication. It serves as a
barrier to prevent the gastric acids in the stomach from dissolving or degrading drugs
after you swallow them.
(ii) Extended release: ER forms are designed to make them last longer in your body.

b) Sublingual: Placement under the tongue allows a drug to diff use into the capillary network
and, therefore, to enter the systemic circulation directly. Advantages include: it allows the drug
to diffuse into blood circulation directly, Low incidence of infection, Rapid absorption bypass
the GIT environment and the FirstPass metabolism, Disadvantages: Taste, lack of cooperation,
difficulties in co-ordination, and keeping medication at the site of absorption as well as risk of
choking and aspiration could be some disadvantages of sublingual administration in young
children

Example: Misoprostol to reduce postpartum hemorrhage and blood loss during hysterectomy,
nifedipine for hypertensive urgency.

c). Buccal: Convenient route and painless administration, facility to modulate the selection of
excipients, versatility in the design of multidirectional or unidirectional release systems for local
or systemic action, and a predictable drug concentration in the blood. Eating, drinking, or
smoking, can affect how the drug is absorbed and how well it works. Also, these forms don't
work for drugs that need to be processed slowly by your system, such as extended-release
formulations.
Example: Buccal delivery systems include mouthwashes, sprays, chewing gums, bioadhesive
tablets, gels, and patches.

2 ) Parenteral: The parenteral route introduces drugs directly across the body’s barrier defenses
into the systemic circulation. Parenteral administration is used for drugs that are poorly absorbed
from the GI tract.
Advantages
  Can be used for drugs that are poorly absorbed, inactive or ineffective if given orally.
 The IV route provides immediate onset of action.
 The intramuscular and subcutaneous routes can be used to achieve slow or delayed onset
of action.
 Patient concordance problems can be avoided.
Disadvantages
Parenteral preparations to the patient include lack of drug reversal, risk of infection and emboli,
risk of hypersensitivity reactions, and cost.

a.) Intravenous: . IV injection is the most common parenteral route. For drugs that are not
absorbed orally. Advantages include: Drug is delivered immediately upon the completion of a
response requirement and since delivery is into a vein, there is a rapid onset of drug effects. Such
immediacy results in rapid acquisition and strong maintenance of behavior. Disadvantages
include: A vein can be damaged during injection or by the use of an IV catheter line. This can
cause infiltration. When this occurs, medication leaks into surrounding tissue instead of going
into your bloodstream. Infiltration can cause tissue damage.
Example: Antibiotics such as vancomycin, meropenem, and gentamicin. antifungal drugs such
as micafungin and amphotericin. pain relief medications such as hydromorphone and morphine.
drugs for low blood pressure such as dopamine, epinephrine, norepinephrine, and dobutamine.
b.) Intramuscular: Drugs administered IM can be in aqueous solutions, which are absorbed
rapidly Advantages are Rapid and uniform absorption of the drug, especially the aqueous
solutions. Rapid onset of the action compared to that of the oral and the subcutaneous routes. IM
injection bypasses the first-pass metabolism of the drug. It also avoids the gastric factors
governing drug absorption. Disadvantages: Persistent pain at the site of injection. Muscle fibrosis
and contracture. Abscess at the injection site.
Example: Antibiotics- penicillin G benzathine penicillin, streptomycin. Biologicals-
immunoglobins, vaccines, and toxoids. Hormonal agents- testosterone, medroxyprogesterone
c.) Subcutaneous (SC): This route of administration, like IM injection, requires absorption via
simple diffusion and is somewhat slower than the IV route Advantages include: it reduces patient
dependency on hospital facilities and results in reduced drug delivery-related healthcare costs
and resource use. It is also less time-consuming and minimizes the discomfort associated with
intravenous infusion. Disadvantages: Improper subcutaneous injection of pharmaceuticals may
result in side effects, such as bruising, hematoma and pain at the injection site
Example: insulin, heparin, vaccines and some hormones, are commonly administered by
subcutaneous injections
Pharmacodynamics
 References
Goodman & Gilman’s The Pharmacological Basis of Therapeutics by. Joel Griffith Hardman,
Lee E. Limbird, Alfred G. Gilman. 10th Ed.
I. (n.d.). Pharmacology Education Project. Retrieved May 4, 2018, from
https://www.pharmacologyeducation.org/clinical-pharmacology/clinical-pharmacokinetics
Ratain, M. J. (1970, January 01). Principles of Pharmacokinetics. Retrieved from
https://www.ncbi.nlm.nih.gov/books/NBK12815/
Baali, J. J., A., D., S, D., Carter, D., & Mehta, A. (2011, April 10). Pharmacokinetics Basics-
Absorption, Distribution, Metabolism and Excretion | Notes. Retrieved from
https://pharmaxchange.info/2011/04/pharmacokinetics-basics-absorption-distribution-
metabolism-and-excretion/
Edge Hill University. Pharmacokinetics_and_Pharmacodynamics_the_basics [PDF] (1st ed., pp.
19-24). Ormskirk. Retrieved from
https://www.associationforprescribers.org.uk/images/Pharmacokinetics_and_Pharmacodynamics
_the_basics.pdf