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Intranasal Transmucosal Drug Delivery
Intranasal medication is a procedure for administering medications through the nasal passages. Also known as transmucosal administration or nasal drug delivery, intranasal medicating employs an atomization device that fragments the medication into fine particles as it is being sprayed into the nose. This method of administration offers several advantages. This article will examine these advantages as well as what medications are commonly dispensed using this method.
The use of nasal administrated medications offers 6 key advantages. Nasal administration provides a direct route for medications, avoiding gastrointestinal destruction and hepatic first pass metabolism. Transmucosal medicating effectively increases bioavailability while decreasing time of onset. The process is easy to use and safe. We will explore these six advantages in more detail below.
Nasal administration is a nose-brain pathway for a much more rapid dispersal. The olfactory mucosa is in direct contact with the brain and cerebrospinal fluid (CSF). When medications are absorbed through the olfactory mucosa, they are directly transported to the CSF. This nose-to-brain pathway offers a rapid and direct route for medication deliver to the brain.
Drugs administered orally are absorbed through the gastrointestinal tract. While enroute, the drug can be significantly degraded by gastric acidity, intestinal membrane enzymes, complexion with food constituents or bacterial enzymes. Oral medications sit in the stomach for 30 to 45 minutes before being sent to the intestines for absorption. After absorption into the blood, the medication is delivered to the liver for detoxification. This time consuming digestive process destroys much of the medication before it reaches the blood stream for dispersal throughout the body. While oral administration remains the most convenient delivery method, it provides very little absorption and transfer of the drug to the blood stream.
Hepatic First Pass Metabolism
Nasal medication bypasses first pass metabolism while oral medications do not. As mentioned above, all blood from the intestines is routed to the liver for detoxification. The liver metabolizes around 90% of oral medications before the medication reaches the heart. This leaves very little of the drug remaining after liver detoxification for patient use. A nasal administered drug; however, absorbs directly into the veins through the nasal mucosa; therefore, by-passing first pass metabolism. The heart then pumps the drug to the entire body without delay.
Bioavailability refers to the amount of drug transmitted into the bloodstream. For instance, IV administered medications have 100% bioavailability while most oral medications have only around 5 to 10% bioavailability. The bioavailability of nasal medications is dependent upon molecule size and pH of the medication. For instance, Nalozon, a poplular intranasal medication, has 90+% bioavailability while midazolam has 75+% Nalozone and Fentanyl has 80+%. Transmucosal administration is generally more effective than subcutaneous or intramuscular injections.
Time of Onset
Intranasal administration is rapidly effective with an onset time between only 2 to 10 minutes.
Ease of Use
Nasally administered drugs are convenient and easy. The administration is painless and does not expose the patient or caregiver to accidental needle sticks. Waste is reduced without the need for sharps containers and hazardous disposal. Intranasal administration is safe for the patient with no high peak serum levels. Nasal administered drugs are safer to use for violent individuals or for seizure victims. Various medications may be delivered to the patient in any position, whether sitting, lying down, prone, on side or upside-down. Since nasal administration takes only a second to administer the patient may not need to be restrained.
Types of Nasal Mucosa Administrations
Nasal administrations may take the form of spray bottles, nose droppers, pressurized aerosol or atomized unit dose sprays. The latter is the most effective method. Spray bottles fail to provide a consistent dosage and often results in excessive amounts of the drug draining into the throat. Large particles of the medication can also form deposits on the nasal mucosa. Nose droppers often produce the same unwanted results as spray bottles with much of the medication not being absorbed and draining into the throat. Pressurized aerosol devices tend to break the medication into smaller particles that flow down to the lungs which offer less effectiveness with absorption and may result in respiratory complications.
Atomization of the medication reduces the particles into 2 to 10 micrometers that provide for optimal absorption through the nasal mucosa. The mucosa offers a large surface area of more than 180 square centimeters of highly vascularized tissue. This area has more blood vessels per gram of tissue than in muscle tissue, the brain, or even the liver. Absorption through the nasal mucosa offers the best results for rapidity and efficacy. Atomization best reduces the medication particles to the optimal size for absorption. Additionally, because the medication is atomized into a mist form, it less is likely to be expelled from the nose into the external environment.
Nasal Medication Delivery Devices
There are several manufacturers that make nasal medication devices. Below is a list of the bestselling devices listed alphabetically.
- Accuspray by Becton Dickenson - offers patients a less invasive drug administration. Designed for use by both doctors and patients, Accuspray is easy-to-use with no pre-activation or loading required. The drug to be administered is clearly visible, allowing visual inspection of the medication before administration. Accuspray provides for the administration to be easily divided, allowing the drug to be delivered to each nostril to access more mucosa membrane for better dispersal.
- Carpuject by Pfizer - Carpuject has a compact design that is needleless and prevents injuries. The Carpuject syringe system can dispense a wide variety of medications with easy-loading cartridges. Caregivers enjoy the easy one-handed operation and disposal.
- OptiNose - The OptiNose nasal device is designed to treat chroinic nasal inflammatory diseases, migraines, and Autism Spectrum disorder. OptiNose provides two separate delivery devices designed to administer either powder and liquid medications. The devices minimize local irritation and allows patients to self-medicate.
- MAD Intranasal Mucosal Atomization Device by Teleflex – This nasal atomization device is designed to be used with drugs approved for intranasal delivery. It requires no sterile procedures, is painless, and is quick and easy to administer. The atomized medication is rapidly absorbed across the mucosal membranes directly into the blood stream for greater bioavailablity.
- CPD by Kurve Technology - This nasal atomization device is non-invasive and provides controlled particle dispersion to deliver medications directly to the brain. The CPD nasal drug delivery system can control the size of the liquid droplets down to 1 micron regarless of the viscosity of the formulation.
- DirectHaler by Acerus Pharma - The DirectHaler is also known as the Direct-Haler and is a nasal drug delivery device designed to use the patients breath to disperse dry powered medications to the patient. Recently, the Acerus Pharmaceutical Corporation has acquired this award-winning intranasal drug delivery device from a company in Denmark.
- VeriDoser by Mystic Pharmaceuticals - The VeriDoser offers nasal drug delivery with precise, calibrated dosing. Mystic's VeriDoser requires no priming and has a dose counter. The spray plume is configurable into steam, spray or aerosolized spray. The design accommodates proteins, peptides and stem cells formulations to treat CNS, neurodegenerative disorders, brain tumors, HIV encephalopathy, epilepsy, Huntington, Alzheimer's and Parkinson.
Common Medications Dispensed Using Nasal Atomization
Nasal atomization delivery is being developed for many applications, including Alzheimer's, Parkinson's, brain tumors, diabetes, multiple sclerosis, schizophrenia, pain control, and migranies. Below is a list of the most popular drugs currently dispensed by intranasal administration grouped by treatment type.
Pain Control - Opiates
Sedation - ά-2 Agonists
Seizure Therapy – Benzodiazepines
Reversal of Conscious Sedation
Angina (Chest Pain)
Specific Nasal Drug Delivery Administrations
Fentanyl is an opiate used for pain control and is an ideal drugs for use with intranasal administration. A prescription is required for this drugs. Fentanyl has a rapid onset and short duration and is one of the strongest opiate drugs sold on the market. Intranasal fentanyl is rapidly absorbed, reaching maximum concentration in just 4 to 11 minutes. Bioavailability is around 71% but appears to be pH dependent with increased bioavailability associated with higher pH. 1
Ketamine is a dissociative anesthetic opiate that is often used for treatment-resistant depression. Beside IV administration, intranasal is the second most common method of dispensing Ketamine. Intranasal administration requires less skill to use and offers less risk to the patient. However, many patients report that infusion offers more relief and lasts longer while intranasal is less expensive and more convenient. 2
Midazolam produces sleepiness or drowsiness and helps relieve anxiety. It also produces amnesia so that the patient will forget any discomfort or pain that may occur following surgery. In intensive care hospital situations, Midazolam is used to induce unconsciousness. This drug is also used to treat epilepsy and seizures. Midazolam requires a prescription and close doctor supervision. Intranasal midazolam was found in a study to have the same efficacy as IV administrations but that the short administration time for nasal as opposed to IV set up favored the use of nasal delivery. 3
Narcan is an FDA-approved drug known as naloxone hydrochloride. This drug is an opioid antagonist used for the emergency treatment of individuals with respiratory or central nervous system failure due to opioid overdose. Administration of naloxone by nasal spray atomization is easy and convenient and offers increased efficacy. Narcan nasal spray is designed to provide a singe 4 mg dose. Administration of the drug using a Narcan MAD Syringe allows the medication to be atomized for quick metabolism. 4 The LMA MAD Nasal Intranasal Mucosal Atomization Device from Teleflex is specifically designed for administering this lifesaving drug.
First Responders Use of Intranasal Naloxone
Emergency Medical Technicians (EMT) and ambulance crews have found the use of narcan nasal spray to restore spontaneous respiration for drug overdose patients in just a matter of seconds. Ease of use without the risk of needlestick injury are cited as primary benefits. The requirement for minimal training has also been cited as a benefit. Some have advocated extending the use of Narcan nasal sprays to community workers that often come into contact with drug abusers. 5Some police departments are now equipping officers with opioid-overdose antidote because the police are often the first on the scene.6 The U.S. Attorney General Eric Holder advocates that the police and fire departments should equip their first responders with naloxone to save drug overdose victims.7
Parental Use of Nasal Nacan
Some states are allowing Naloxone to be sold at drug stores without a prescription in an effort to curb teenage overdose deaths. 8
Nasal Narcan Studies
- Barton, Erik D., et al. "Efficacy of intranasal naloxone as a needleless alternative for treatment of opioid overdose in the prehospital setting." The Journal of emergency medicine 29.3 (2005): 265-271.
- Kerr, Debra, et al. "Randomized controlled trial comparing the effectiveness and safety of intranasal and intramuscular naloxone for the treatment of suspected heroin overdose." Addiction 104.12 (2009): 2067-2074.
- Kelly, A., and Z. Koutsogiannis. "Intranasal naloxone for life threatening opioid toxicity." Emergency medicine journal: EMJ 19.4 (2002): 375.
1Foster, David, et al. "Pharmacokinetics and pharmacodynamics of intranasal versus intravenous fentanyl in patients with pain after oral surgery." Annals of Pharmacotherapy 42.10 (2008): 1380-1387.
2"Route of Administration: Critical to Achieving Relief." Ketamine Advocacy Network. N.p., 2015. Web. 30 Aug. 2016.
3"Therapeutic Intranasal Drug Delivery." Treating Seizures with Intranasal Medications. N.p., n.d. Web. 30 Aug. 2016.
5Strang, John, et al. "Clinical provision of improvised nasal naloxone without experimental testing and without regulatory approval: imaginative shortcut or dangerous bypass of essential safety procedures?." Addiction (2016).
6Fuller, Steve. “City police make first Narcan save." The Ellsworth American. August 24, 2016.
7Sledge, Matt. “Eric Holder Calls On First Responders To Carry Naloxone, Anti-Overdose Drug." The Huffington Post. April 16, 2014.
8Fiangan, Katlin. “Narcan to Be Sold at Pharmacies Without Prescription in Vermont." NECN.com. August 25, 2016.
Other Applicable Studies of Using Intranasal Administration
- Barton, Erik D., et al. "Efficacy of intranasal naloxone as a needleless alternative for treatment of opioid overdose in the prehospital setting." The Journal of emergency medicine 29.3 (2005): 265-271.
- Jain, Kewal K. "Drug delivery systems-an overview." Drug delivery systems (2008): 1-50.
- Hussain, Anwar A. "Intranasal drug delivery." Advanced drug delivery reviews 29.1 (1998): 39-49.
- Pires, Anaísa, et al. "Intranasal drug delivery: how, why and what for?." (2009).
- Reger, M. A., et al. "Effects of intranasal insulin on cognition in memory-impaired older adults: modulation by APOE genotype." Neurobiology of aging27.3 (2006): 451-458.
- Wermeling, Daniel P., and Jodi L. Miller. "Intranasal drug delivery." DRUGS AND THE PHARMACEUTICAL SCIENCES 126 (2003): 727-748.
- Wolfe, Timothy R., and Tony Bernstone. "Intranasal drug delivery: an alternative to intravenous administration in selected emergency cases."Journal of Emergency Nursing 30.2 (2004): 141-147.
- Zia, H., P. Dondeti, and T. E. Needham. "Intranasal drug delivery." Clinical Research and Regulatory Affairs (2008).
Burt Cancaster, Author
After a long winter, millions with physical disabilities or long-term illnesses are eager to get out of town -- or the country. With just a little planning, bringing along an oxygen therapy device, special medicine or mobility aid is a breeze. Planning will also make your trip that much more enjoyable because you will have the same wellness and mobility that you do at home.
First Things First: Know Before You Go
Beyond financially planning for contingencies like a minor mishap or gotta-have-it impulse purchases, ask your hotel the right questions ahead of time:
- Will my room be wheelchair accessible?
- Is there a working elevator?
- Does the pool area have a lift?
- How wide are halls and door entries? Will a wheelchair or mobility scooter fit?
- Is there a working ice machine to keep medicine cool? Are rooms available with mini-fridges for sensitive medication?
- Ask your pharmacist what medicine alternatives are available if heading overseas -- just in case. Also, budget in the costs in case insurance won't cover expenses abroad.
Make a checklist of pertinent questions and avoid the siren song of discount rooms online -- do your homework and call before booking!
Let's Get Packing
Lay out your medicines and make a daily dosing protocol list to stay on top of them -- especially if traveling through multiple time zones in one day. Do you use medication that requires multiple accessories like insulin? The right kind of pouch, such as Medicool's Dia-Pak Deluxe Diabetic Travel Bag, has thoughtful features to help you organize up to two weeks' worth of supplies. Don't forget to pack items, such as the LifeScan Logbook Diabetic, that help you maintain a proper regimen despite the rigors of travel.
Hit the Road, Jack
The oil's been changed, wiper blades have been checked and the fossilized French fries have been vacuumed out -- the car's ready to roll; right? Maybe, but a few economical items will make the most of every road trip. Stander's Automobility Solution, for instance, features a clever swivel seat that enables occupants to twist and pivot in/out of a car. The kit also includes a handle that mounts tool-free to a vehicle's door latch for additional stability during vehicle ingress/egress.
Between convenience store pizza and 64-ounce fountain drinks, sickness and gotta-go moments can strike anyone -- at any time. Keep your vehicle's interior pleasant and sanitary with conveniences such as a Car Sick Kit with a special bag that locks in odors or NuHope's Travel Urine Collector that aids ostomy and catheter users when rest stops are few and far between.
Major U.S. airlines are very sensitive to passengers traveling with a Portable Oxygen Concentrator. However, there are a few guidelines they, and we, like to remind passengers of:
- Battery life -- Oxygen Therapy patients must have a battery life that is equal to 1.5 times (or 150%) of the scheduled flight time. This ensures that portable oxygen concentrators have power for unexpected delays or diversions.
- Ask, ask, ask -- Before booking, call your carrier's customer service division to ask about special protocols they may have for on-board oxygen concentrator use.
If traveling internationally, Vitality Medical advises you to check with us or your machine's manufacturer about overseas usage because this may void the factory warranty. Select machines may not be compatible with European- or Asian-market power outlets and may require an additional adapter or alternative plans if overseas usage is impossible.
If taking your oxygen concentrator on the road or overseas isn't a possibility, Vitality Medical has a rental program that supports your wanderlust. Several different brands are available and dedicated Oxygen Concentrator Specialists will provide support and oversee shipping logistics.
All Roads Lead to...
Several clever mobility accessories support all travelers, provide stability and discreetly tuck away once you reach your destination.
Visiting a relative without a ramp? No sweat! A travel-ready wheelchair/scooter ramp from Drive Medical will put everyone at ease, protect your host's home and let you focus on visiting. Several innovative walking aids out there help you make the most of tours, museums and gallery strolls. These include Medline's Folding Aluminum T-Handle Cane that cane that folds into a compact, ready-to-store unit when you reach your destination. Another handy item is Mountain Properties' Elite Walking Cane that features a fold-out seat with three legs for stability, making sure you always have a place to rest.
Spring's arrival means you'll likely be off to see dads and grads, so make sure you're ready. A little planning ahead of time means a physical disability or illness won't stop you from enjoying our big, beautiful world!
To a life full of Vitality!
According to the American Diabetes Association, an estimated one in five people with diabetes seek medical help, particularly for foot problems. A person who has diabetes is more susceptible to foot problems because diabetes damages the nerves and reduces blood flow to the feet, making it harder for your body to heal any injury or cure any infection which might make your feet vulnerable.
Proper foot care is essential for people who suffer from diabetes and with an estimated 25.8 million diabetics living in the United States alone, it is necessary to know the steps to avoid any serious foot problems.
This is a simple routine which everyone should follow. Keep your feet clean by washing them several times a day. If they are clean and not covered in any dust or dirt, you will reduce your chances of suffering from foot-related infections. Take special care when washing and dry the gaps between your toes to ensure that moisture isn't left behind in the crevices.
Many people forget that our feet need as much moisture as the rest of our body, so apply a thin layer of lotion to the top and bottom of your feet. Just a few seconds of diabetic skin care can keep your feet comfortable and healthy. Keep your feet clean, smooth and moisturized.
2.Don't soak your feet
Soaking our feet might feel good during a pedicure but studies show that soaking our feet for prolonged periods of time can dry out the skin and cause cracks, which can lead to harmful infections. Soak your feet in clean warm water for a short time only to take away the stress and to relax your foot muscles.
3.Regular blood flow
Perform some small foot exercises such as wiggling or rotating the ankle for a good five minutes to keep the blood circulation normal in your feet. While sitting, put your feet up instead of crossing your legs or just letting them hang.
4.Trim your toenails with caution
Having trimmed and clean toenails is a must, so always use clean nail cutters. Cut the nails straight across to avoid ingrown nails. If you can't cut or trim your own toenails, always ask for help.
5.Keep your feet away from heat
Avoid contact with heaters, electric blankets, hot water bottles or any material which might bring heat to your feet. Warmth can cause burns on your skin and other injuries. Too much heat exposure can cause decreased foot sensation as well. Always keep your feet away from anything which might cause excessive heat.
6.Wear proper shoes
Correct diabetic foot wear is necessary for everyone. Having the right size shoes which are made of comfortable material are a must, which means you shouldn't compromise just for the sake of fashion. Avoid walking barefoot and wear shoes which ar comfortable for you.
To keep your feet healthy, you should wear diabetic socks. There are socks that are specifically designed for people with diabetes which are made from acrylic fibers and free of any dyes that might cause irritation. Acrylic socks are better than cotton at keeping excess moisture away from the skin.
8.Check your feet daily
Perform a proper inspection of your feet daily, making sure that the condition of your feet is healthy so that you can catch any irregularities before they become a problem.
9.Check with the doctor
The best way to avoid any problem before it becomes a complication is by preventing it from happening. If the doctor has given you any precautions, follow them properly. Work with your healthcare providers and keep an eye on your blood sugar to stay within range. If there is any problem or if there are any changes, notify your doctor immediately.
The best way to lead a healthy life is by knowing how to take care of your own self. Diabetes might be a problem but that doesn't mean you should stop living and only think of the consequences. Proper foot care is essential for a diabetic and by following these simple instructions, you can live your life with the knowledge that you are doing everything to stay happy and healthy.