INTRODUCTION TO THERAPEUTICS

CONTENT OUTLINE
By the end of this lecture, a student should be
able to;
Define the term therapeutics
Roles of pharmacy practitioner in the health

care team.
EXPECTATIONS
 Description/Definition

 Presentation (Signs and symptoms

where applicable),

 Predisposing factors where applicable

and

 Management (Just stating the

pharmacological and non-
pharmacological management where
applicable)
 Therapeutics

 Def, therapeutics is defined as a branch that

deals specifically with the treatment of
diseases and the art and science of healing.
 In pharmacology, therapeutics refers to the
use of drugs and the method of
administration in the treatment of disease.
 Roles of pharmacy
practitioner in the health
care team
The role of pharmacy
professionals in health care

 Processing of prescriptions
◦ Verifies legality, safety and appropriateness
◦ Check patients medication records before dispending
◦ Ensure accuracy in dispensing

 Care of patients/clinical pharmacy

◦ Collect and integrate information about patient drug
history
◦ Advises patients on drug related precautions
◦ Monitor and evaluate therapeutic responses
 Monitoring of drug utilization
◦ Practice research projects for schemes to analyze
prescriptions for the monitoring of adverse drug reactions

 Providing drug information necessary to other health

professionals and patients to promote rational use of dugs .

 Extemporaneous preparation and small

scale manufacture of medicines
◦ Aim to adopt formulations to the need of individual
patients
 Traditional and alternative medicines
◦ Supply of traditional medicines and homeopathic
prescriptions

 Responding to symptoms or minor ailments

◦ Handling of symptoms or minor ailments
◦ Pharmacist may respond without supply of medicines

 Informing health care professionals and the public

◦ Informing health professionals about existing and new
medicines
◦ Promote rational drug use among health professionals
and patients
 Health promotion
◦ Participate in sensitizing communities locally or
nationally on health related issues such as:
rational drug use, alcohol abuse, tobacco use
etc.

 Regulatory control and drug management by participating in

implementation of drug policies
 Industrial pharmacy practice by ; registration of drugs,
conducting clinical trials and post marketing surveillance.
 Academic activities involving training students in colleges and
universities preparing them to offer pharmacy services to the
public.
 Domiciliary services
◦ Providing advisory and supply services to
residential homes for the elderly and long term
patients

 Agricultural and veterinary practice

◦ Pharmacists supply animal medicines and
medicated animal feeds
Reference materials
 Winfred, A.J. and Richard, M.E. (2005).
Pharmaceutical practice. 3rd ed.
 Stone, P. and Curtis, J.S. (1998). Pharmacy
practice.
 Management sciences for health by who, (2014)
 The internet
DRUG INTERACTIONS

BY
OKIDI OSCAR P’OKELLO
Outline
 Drug interactions
◦ Definition
◦ Clinical relevance
◦ Types

 Factors predisposing to drug interactions

 Impact of drug intereactions

 Def. A drug interaction occurs when
the effects of one drug is affected by
the presence of another drug, food,
drink or an environmental chemical
agent.

◦Alteration of effect of one or more

drug or the production of idiopathic
effects
Clinical relevance
 Identificationof factors affecting the
risk of drug interaction

 Identification
of Patients likely to be
adversely affected by a drug
interaction
Factors affecting the risk of drug
interaction
 Poly pharmacy ; the more drugs a patient
takes the greater is the likelihood of a drug
interaction
 Organ functioning of a patient –particularly
the liver and the kidney
 Drug administration
 Duration of therapy
 Number of prescribers for a particular
patient and their level of coordination
Patients likely to be adversely affected
by a drug interaction

 The elderly or seriously ill patients

 Patients on long term therapy in chronic

disease e.g. HIV patients

 Patients undergoing complicated surgical

procedures
TYPES / MECHANISMS OF
DRUG INTERACTIONS
Two mechanisms of interaction
 Pharmacokinetic
 pharmacodynamics
Pharmacokinetic: One drug
affects the process by which the drug
is absorbed, distributed, metabolized
or excreted.

 There is an increase or decrease in

the amount needed to produce
pharmacological action
Pharmacodynamic
 These are interactions between drugs
which have similar or antagonistic
pharmacological effects or side effects.

 They may be due to competition at

receptor sites or occur between drugs
acting on the same physiological
system.

 They are usually predictable from a

knowledge of the pharmacology of the
interacting drugs.
NOTE
 Object drug: one whose activity is affected
by an interaction

 Precipitant drug: it precipitates the

interaction
 Pharmacokinetic
Pharmacokinetic effects may be on
i) Absorption
 Complexation and adsorption

 Alteration of GI PH
 Alteration of GI micro flora- dioxins is substantially inactivated by
the GI bacteria in about 10% of individuals. A broad spectrum
antibiotic therefore ↑bioavailability.
 GI motility; altering the rate of stomach emptying affects
absorption of drugs which are absorbed in the upper part of small
intestines and can reduce absorption of e.g. levodopa by 50%
◦ Slows (e.g. atropine, opiates)
◦ Accelerates (e.g. Metoclopramide)
ii) Distribution
 Displacement: On protein binding – relative
affinities for plasma proteins.

One drug can displace another there by

increasing its proportion to diffuse form for
plasma to its site of action.

NOTE: The les bound a drug is, the more

efficiently it can traverse cell membranes or
diffuse.
iii) Metabolism

 Many drugs are metabolized in the liver.

 Induction of the hepatic microsomal enzyme by one

drug can gradually increase the metabolism of
another.

 Inhibition of the hepatic microsomal enzyme by one

drug can gradually decrease the metabolism of
another.

 Although there is an overlap ach CYP isoenzyme tends

to metabolize a discrete range of substances.

 The genes for isoenzymes vary between individual

and, sometimes ethnic groups which may affect
iv) Renal excretion

 Changes in the active tubular secretions

 Alteration in urinary PH

 Blood flow alteration

 Competition occurs between drugs which

share active transport mechanisms in the
proximal tubule. E.g. Salicylates and some
other NSAIDS delay the excretion of
methotrexate lading to serious methotrexate
toxicity.
Some drug substrates, inducers and inhibitors of hepatic

hepatic isoenzymes
substrates
CYP1A2
amitryptyline CYP2C19 CYP2C9 CYP2D6 CYP2E1 CYP3A4
caffeine amitryptyline amitriptyline amitryptyline acetaminophen
alprazolam
clozapine citalopam colecoxib clomipramide clozatazone asfemizole
cycclobenzapine lomipramine diclofenac codeine daspone
buspirone
fluvaxamine cyclophosphamide lurbiprofen despramine enflurane Ca²+
blockers
imipramine diazepam ibuprofen dextromethorphan ethanol
carbamazepine
mexiletine imipramine losartan imipramine halothane cloapride
olanzapine melfinavir phnytoin nortriptyline isoniazid doxorubicin
propranolol omeprazole piroxicam oxycodone
tacrine phenytoin sulfamethoxazole paroxetine etopoide
R-warfarin S-warfarin thioridazine fentanyl
theophylline citaloprim tobutamide risperidone folodipine
timol HIV protease inhibitors
veriflaxine
ifosphamide

lavostatin

midazolam

nifedipine
pimozide
quinidin
quinine
inhibitors of the isoenzymes
cemetidine cemtidine amidorane amidorane disulfiram amidarone
ciprofloxacin felbamate fluconazole clorpheniramine water cress cemetidine
citalopram fluoxamine fluoxetine fluoxetine cemetidine cyclosporine
diltiazem ketoconazole fluuvastatin haloperidol danazol
encoxacin lansoprazole isoniazid indinavir diltiazem
erythromycin omeprazole metronidazole paroxetine fluconazole
mefletine ticlopidine phenylbutazon quinidine grape fruit juice
ofloxacin septrin ritonavir HIVproteaseinhibitors
ticlopidin ticlopidine thioridazole ketoconazole
fluvoxamine ticlopidine macrolides
(not azithromycin)
Miconazole
Nefazadone
Omeprazole
Quinine
Ritonavir
Verapamil

eythromycin
Inducers of the isoenzymes
Carbamaazepine carbamazepine Phenobarbital chronic ethanl carbamazepine
Tobacco norethindron rifampicin soniazid riabutin
omeprazole rifampicin Secobarbital tobacco rifampin
ritonavir
Pharmacodynamics
 Pharmacodynamics effects may be;
 Agonism/antagonism
 Addition /summation
 Synergism/potentiation
 Important PD Interactions
Drug Interacting drugs Mechanism Effect
/ disease states

Salbutamol Beta-blockers Beta agonist and Diminished efficacy

beta antagonist of beta agonist

Digoxin Loop and Diuretics ↓ K+ ↑ potential for

thiazide diuretics digoxin toxicity

Nitrates Sildenafil Both ↑ cAMP ↑ vasodilation and

concern of ↓ BP
Warfarin Vitamin K Warfarin prevents Large amounts of
vitamin K from vitamin K will ↓
being used to warfarin efficacy
make clotting
factors
NSAIDS Hypertension NSAIDs cause fluid BP ↑
(e.g. retention
ibuprofen)
Factors predisposing to drug
interactions
Clinical sources
 Polypharmacy; the more drugs a patient takes
the greater is the likelihood of a drug
interaction

 Narrow TW requiring careful dose control

 Drug either an inducer or inhibitor of liver

enzymes

 Use for a long period of time

 Drugs which exhibit zero-order kinetics

Patient factor
 Multiple drug therapy

 Severe illness

 Organ functioning of a patient –particularly the

liver and the kidney. Pts with impaired
renal/hepatic function

 Age; elderly and young

 Co-morbid patients


 Impacts / Outcomes
 Loss of therapeutic effect of one or
all drugs

 Increased pharmacological activity of

one

 Increased toxicity of one drug

 Organ dysfunction / failure

 Counteracting drug interactions
 Practitioners should be continually alert to the
possibility of drug interactions and take
appropriate steps to minimize their occurrence.

 Incase the combination of potentially interacting

drugs is unavoidable, the dose of the drug likely
to have increased effects as a result of the
interaction should be reduced

 Management of the side effects of interaction

 Avoid concomitant administration

 Individualize patients therapy

 Counteracting drug interactions
 Patients education

 Always ask for non prescription medicines

 Modify dose of one of the interacting drug

 Patient taking a combination of potentially

interacting drugs should be monitored for toxic
effects using clinical variables or plasma drug
levels for at least 2 weeks or until they are
stable

 It may be appropriate to switch one of the

treatment to one which doesn’t interact.
 HOME WORK

 Mechanisms of drug interaction with

examples, stating the object drug and
precipitant drug.