Intranasal Medications in clinical practice

Slides:



Advertisements
Similar presentations
INTRA-NASAL DRUG DELIVERY SYSTEM
Advertisements

Intranasal Medications in the Prehospital Setting
Intranasal Medications in Hospice
HOW DO DRUGS GET INTO THE BODY?. WHY BE CONCERNED ABOUT HOW DRUGS GET INTO BODY? Bioavailability - % of dose that gets into body Bioequivalence - similarity.
2014 EMR Naloxone Presentation DPH/EMS Program Wisconsin Department of Health Services Naloxone Intranasal Administration in the Pre-hospital Setting –
Administration and Absorption of Drugs. Factors that effect the action of a drug 1.Rate of accumulation at its site of action 2.Concentration of the drug.
Lecture 4.
Region 6 Protocol Update 2014 Pharmacology Presence Regional EMS.
Drug Administration Lesson 3. Definitions n Pharmacokinetics l What the body does to the drug. l Administration, absorption, distribution, & fate l Focus.
Drug Schedules. Goal: to organize the control of drugs under 5 classifications (schedules of controlled substances) Potential for abuse Accepted medical.
Preparing and Administering Medications
Principles of Pharmacology. SOURCES AND NAMES OF DRUGS Sources of Drugs Many drugs are isolated from plants or chemically derived from plant substances.
General Pharmacology CHAPTER 16. Pharmacology: The science that deals with the origins, ingredients, uses and actions of medical substances.
Intranasal Medications in the Prehospital Setting.
Pharmacokinetics Chapter 4.
2014 Intranasal Pilot DPH/EMS Program Wisconsin Department of Health Services Naloxone Intranasal Administration in the Pre-hospital Setting – Basic Life.
A Brief Introduction to Intranasal Medications
Routes of Drug Administration
Pharmacokinetics (PK): What the body does to the drug? Most drugs: Enter the body by crossing barriers Distributed by the blood to the site of action Biotransform.
Vn117 animal nursing.   Prevention of injury by drugs  Prevention of injury by admin equipment  Correct storage of drugs  Correct admin methods for.
Pharmacology Department
Limmer et al., Emergency Care, 11th Edition © 2009 by Pearson Education, Inc., Upper Saddle River, NJ DOT Directory Chapter 15 General Pharmacology.
ADME And PHARMACOKINETICS.
Methods of Drug Delivery
© 2004 by Thomson Delmar Learning, a part of the Thomson Corporation. Fundamentals of Pharmacology for Veterinary Technicians Chapter 4 Pharmacokinetics.
Lecture 2.  Clearance Ability to eliminate the drug  Volume of distribution (Vd) The measure of the apparent space in the body available to contain.
Routes of Drug Administration
Tutorial 1 January 18, 2013.
Bioavailability Dr Mohammad Issa.
Modelling and Simulation Group, School of Pharmacy Intranasal Fentanyl in a Nutshell Aaron Basing.
Pharmacology Department
PHARMACOKINETICS CH. 4 Part 2. GETTING IN ABSORPTION Definition – the movement of a drug from the site of administration into the fluids of the body.
Chapter 4 Pharmacokinetics Copyright © 2011 Delmar, Cengage Learning.
Pharmacokinetics of strong opioids Susan Addie Specialist palliative care pharmacist.
Bledsoe et al., Paramedic Care Principles & Practice Volume 1: Introduction © 2006 by Pearson Education, Inc. Upper Saddle River, NJ Basic Pharmacology.
ADME.
PHARMACOKINETICS Part 3.
Pharmacology I BMS 242 Lecture I (Continued) Introduction; Scope of Pharmacology Routes of Drug Administration Dr. Aya M. Serry 2015/2016.
Pharmacology Ideal Drug  Effectiveness  Safety  Selectivity  Reversible  Predictability  Ease of administration  Freedom from drug interactions.
Chapter 35 Medication Administration. Scientific Knowledge Base To safely and accurately administer medications you need knowledge related to: ◦Pharmacology.
Pharmaceutics I صيدلانيات 1 Unit 2 Route of Drug Administration
Pharmacokinetics I Drug administration and absorption Prof. Hanan Hagar Pharmacology Department.
DRUG ABSORPTION AND DISTRIBUTION OF DRUG
Opiate Analgesic Use in Pediatric Patients Bob Rappaport, M.D. Deputy Division Director Division of Anesthetic, Critical Care and Addiction Drug Products,
Naloxone: Prescribing and Dispensing
Rectal drug administration
 1-What is the best drug to be used?  2-How it is going to be given?
European Patients’ Academy on Therapeutic Innovation Ethical and practical challenges of organising clinical trials in small populations.
Principles of Drug Action
Professor Dr. Nafeeza Mohd Ismail M.B.B.S.(Mal), Ph.D (UKM) Professor of Pharmacology Faculty of Medicine UiTM Drugs and You ASSIGNMENT.
 Parenteral = Injection into body tissues  Invasive procedure that requires aseptic technique  Risk of infection  Skills needed for each type of injection.
OVER THE COUNTER MEDS INTRODUCTION No prescriptions are necessary and no questions need to be answered to attain these drugs OTC med use saves.
Intranasal Drug Deliver – A new way John Mackenzie, June 2010.
routes of drug administration By Hawra alsofi
Routes of drug administration
Route of Drug Administration
Presentation On Routes of drug administration & it’s significance
Introduction; Scope of Pharmacology Routes of Drug Administration
Pharmaceutics 2.
Intranasal Medications in the Prehospital Setting
Introduction; Scope of Pharmacology Routes of Drug Administration
Routes of Drug Administration
Foundations and Principles of Pharmacology
Pharmacokinetics: Drug Absorption
Foundations and Principles of Pharmacology
Introduction to Pharmacology
Pharmacokinetics: Drug Absorption
How and Why Drugs Work PPT Series 5B
Presentation transcript:

Intranasal Medications in clinical practice

Transmucosal medication delivery Is this really a novel idea? Commercially available transmucosal drugs: Actiq oral (transmucosal fentanyl lollipop) Nitroglycerin – Sublingual. Stadol (butorphanol) - Intranasal opiate. Fentora - Transmucosal fentanyl tablet DDAVP - Intranasal delivery route. Migraine medications – Migranol (DHE), etc. Influenza Vaccine - Intranasal system is available. Active area of pharmacology research

Transmucosal Drug Delivery Many IV medications, including analgesics and sedatives, can be delivered transmucosally, though not currently available for that indication commercially: Large literature base to support their use. Generic drugs are available, cutting costs significantly.

Why Intranasal (IN) medications? This delivery route has several advantages: Its easy and convenient Almost everyone has a nose The nose is a very easy access point for medication delivery - even easier to access than IM or IV sites, much easier than rectal delivery No special training is required to deliver the medication No shots are needed Painless Low risk It eliminates any risk of a needle stick to the medical provider

Intranasal Medication Administration Needleless: Intranasal Medication administration offers a truly “Needleless” solution to drug delivery. Superior: Intranasal medication administration generally results in superior drug delivery to the blood stream compared to other transmucosal routes. The remainder of this discussion will surround the topic of intranasal drug delivery issues.

Lecture Outline Part 1: Discuss the concept of “Off-label medication” General principles of intranasal medication delivery Part 2: Intranasal medications in clinical practice EMS Emergency Medicine Anesthesia Hospice

IN medications: Off-label use What is “off-label” use Drugs are approved for specific indications in specific subpopulations by specific route of delivery All other uses are off label Common Examples of “off-label” use: IV lorazepam for status epilepsy in children Most IV drugs given to children (80%), pregnant women Most antidotes for drug overdoses ACLS drugs down an endotracheal tube H2 blockers for allergies

IN medications: Off-label use Why are so many common uses “off-label” It costs about $650 million to bring a drug to market for an indication Once it is on the market, clinicians can use it as they choose for any indication. Unless there is a HUGE financial incentive to seek another indication, the pharma company will not spend the money to get another indication

IN medications: Off-label use Is it OK to use drugs “off-label” Yes – in fact is is expected this will occur and this actually helps advance medical care U.S Supreme court on off-label use: “off-label usage of medical devices is an accepted and necessary corollary of the FDA’s mission”… health care practitioners can “prescribe or administer any legally marketed device to a patient” without limitation or interference.

IN medications: Off-label use Center for drug evaluation and research on off-label use: “Any approved product may be used by a licensed practitioner for uses other than those stated in the product label.” FDA on off-label use: “Off-label use is a well-established principle that has allowed doctors to discover new and beneficial uses” for previously approved drugs.

IN medications: Off-label use Nice summary on the topic from and Australian committee: “Routine off-label use (or on-label use) can be justified if there is high-quality evidence supporting efficacy or effectiveness, and sufficient evidence about the medicine’s safety profile to suggest and overall reasonable benefit –risk for a given clinical context” Conclusion: Off-label use is acceptable. Most intranasal drugs are off-label – but that is OK if they provide justifiable benefits.

Understanding IN delivery: General principles First pass metabolism Nose brain pathway Lipophilicity Bioavailability

First pass metabolism Molecules absorbed through the gut, including all oral medications enter the “portal circulation” and are transported to the liver. Liver enzymes then break down most of these drug molecules and only a small fraction enter the body’s circulation as active drug. This process is called “First Pass Metabolism.” POINT: Nasally delivered medications avoid the gut so do not suffer first pass metabolism.

First pass metabolism

Nose brain pathway The olfactory mucosa (smelling area in nose) is in direct contact with the brain and CSF. Medications absorbed across the olfactory mucosa directly enter the CSF. This area is termed the nose brain pathway and offers a rapid, direct route for drug delivery to the brain. Olfactory mucosa, nerve Brain CSF Highly vascular nasal mucosa

Lipophilicity “Lipid Loving” Non-lipophilic molecules Cellular membranes are composed of layers of lipid material. Drugs that are lipophilic are easily and rapidly absorbed across the mucous membranes. Lipophilic molecules Cell Membrane Blood stream

Bioavailability How much of the administered medication actually ends up in the blood stream. Examples: IV medications are 100% bioavailable. Most oral medications are about 5%-10% bioavailable due to destruction in the gut and liver. Nasal medications vary, but when the right drug is delivered in the right way can approach 80%.

Bioavailability Graph demonstrating naloxone serum concentrations when given via IV and IN routes. Note that IV and IN serum levels are similar after about 5 minutes.

Intranasal Medication Administration: Bioavailability Not all drugs can be delivered via the nasal mucosa. Factors affecting bioavailability: Medication characteristics. Medication volume and concentration. Nasal mucosal characteristics. Delivery system characteristics. Mucosal surface area coverage. Medication particle size.

Intranasal Medication Administration: Factors Affecting Bioavailability Medication Characteristics: Drug characteristics that affect bioavailability via the nasal mucosa include: Molecular size. Lipophilicity. pH. Drug concentration. Properties of the solution the drug is solubilized within.

Volume and concentration: Intranasal Medication Administration: Factors Affecting Bioavailability Volume and concentration: Low volume - High concentration. Too large a volume or too weak a concentration may lead to failure because the drug cannot be absorbed in high enough quantity to be effective. Ideal volume for nasal delivery is 1/4 to 1/2 ml per nostril Volumes over 1 ml per nostril are too large and may result in runoff out of the nostril.

Intranasal Medication Administration: Factors Affecting Bioavailability Nasal mucosal characteristics: If there is something wrong with the nasal mucosa it may not absorb medications effectively. Examples: Vasoconstrictors such as Afrin, cocaine prevent absorption. Bloody nose, nasal congestion, mucous discharge all prevent mucosal contact of drug. This might be overcome with suction prior to drug delivery Destruction of nasal mucosa from surgery or past cocaine abuse – no mucosa to absorb the drug.

Intranasal Medication Administration: Factors Affecting Bioavailability Delivery system characteristics: Nasal mucosal surface area coverage: Larger surface area delivery = higher bioavailability. Particle size: Particle size 10-100 microns adheres best to the nasal mucosa. Smaller particles pass on to the lungs, larger particles form drop and rapidly run-out of the nose.

Bioavailability and Particle size Compared to drops, atomized medication results in: Larger surface area of coverage. Smaller liquid particle size allowing thin layer to cover mucosa. Less run-off out the nasal cavity.

Intranasal Medication Administration: Summary Points: Nasal drug delivery is convenient and easy, but it may not always be effective. Nasal drug delivery cannot completely replace the need for injections. Being aware of the limitations and using the correct equipment and drug concentrations will assist you in predicting times when nasal drug delivery may not be effective.

IN drug delivery: Requirements Appropriate Drug Known to be bioavailable across the nasal mucosa Appropriate Concentration Most concentrated form available Appropriate patient Requires treatment Nasal mucosa healthy, free of obvious severe bleeding, thick mucous, etc

IN drug delivery: Conclusions IN drug delivery is: Convenient, easy and effective for selected situations May result in reduced needlestick risk Can improve and simplify your practice and your patients experience Will NOT replace the need for injections

Nasal Drug Delivery: What Medications? There are numerous peer reviewed articles on this topic is you search PubMed or other internet sites for specific indications using key words such as “intranasal” and the medication or application you desire.