Contents Definition Way of Administration Principle Advantage over Buccal route Advantage and disadvantages Types Drugs in the market
Definition Sublingual ( abbreviated SL ), from the Latin for "under the tongue ", refers to the pharmacological route of administration by which drugs diffuse into the blood through tissues under the tongue. Many drugs are designed for sublingual administration, including cardiovascular drugs, steroids , barbiturates , opioid analgesics with poor gastrointestinal bioavailability, enzymes and, increasingly, vitamins and minerals .
Principle When a chemical comes in contact with the mucous membrane beneath the tongue, it diffuses through it. Because the connective tissue beneath the epithelium contains a profusion of capillaries , the substance then diffuses into them and enters the venous circulation. In contrast, substances absorbed in the intestines are subject to " first-pass metabolism " in the liver before entering the general circulation. Sublingual administration ,it ensures that the substance will risk degradation only by salivary enzymes before entering the bloodstream, whereas orally administered drugs must survive passage through the hostile environment of the gastrointestinal tract , which risks degrading them, either by stomach acid or bile , or by the many enzymes therein, such as monoamine oxidase (MAO). Furthermore, after absorption from the gastrointestinal tract, such drugs must pass to the liver , where they may be extensively altered; Video :D
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Advantage over Buccal route
Advantage and disadvantages Advantages Disadvantages Mesenteric circulation is by passed No loss of drug ( by first pass effect ) Higher bioavailability and onset of action (than oral ) Rapid absorption due to high vascularization Reduce side effects due to low dose and high efficiency Fast dissolution and disintegration without water or chewing action Improved drug compliance PH of mouth is neutral so drug will be stable Interferes with eating , drinking and talking Not for Unconscious patients If any is swallowed t hat portion must be treated as an oral dose and subject to 1 st pass effect Only small doses can be accommodated Patient should not smoke while taking the medication as smoking cause vasoconstriction of BV and will decrease the absorption of drug
Types Fast Disintegrating Sublingual Tablets Bio adhesive Sublingual Tablets Thin film Drug Delivery System Lipid Matrix Sublingual Tablets Sublingual Immunotherapy Sublingual vitamin Tablets
Continue Bio adhesive Sublingual Tablets : Water soluble carrier covered with fine particles and a bio adhesive component (applied to extended release tablets ) Sublingual Immunotherapy : ex (allergic rhinitis ) it’s taken as drops or tablets 3 or more times /week , containing a specific allergen which interacts with the immune system to decrease allergic sensitivity (like sensitization) Sublingual Vitamin Tablets : Mainly V.B12 (we must have enough in our bodies )
Drugs In Egyptian and International Markets
Drugs
BUPRENORPHINE An opioid use disorder is a medical condition that is characterized by the compulsive use of opioids .Opioids include substances such as morphine , heroin , codeine , oxycodone , hydrocodone , etc. Buprenorphine sublingual tablet is indicated for the treatment of opioid dependence and is preferred for induction. Prescription use of this product is limited under the Drug Addiction Treatment. Sublingual tablet: 2 mg buprenorphine and 8 mg buprenorphine
Content and the role of each Buprenorphine sublingual tablet is an uncoated oval orange tablet, imprinted with a logo on one side and a numeric imprint on the other side . The tablets contain buprenorphine HCl ( Active Constituent ) Each tablet also contains citric acid anhydrous( disintegrant ) crospovidone (super disintegrant ) FD&C yellow #6 HT aluminum ( Lake : colour ) lactose monohydrate ( Diluent ) magnesium stearate ( Lubricant) mannitol ( Directly compressible Diluent ) pregelatinized starch ( binder) sodium citrate dihydrate .(Alkalizing agent; buffering agent; emulsifier; sequestering agent .)
Isordil ® Sublingual Tablets Isosorbide Dinitrate WHAT ISORDIL IS USED FOR Isordil Sublingual tablets are for the prevention and treatment of attacks of angina. Angina is a pain or uncomfortable feeling in the chest, often spreading to the arms, neck and sometimes to the shoulders and back. The pain may be caused by too little blood and oxygen getting to the heart. Isordil works by opening up blood vessels which allows more blood and oxygen to reach the heart. Isordil may also be helpful in the treatment of some types of heart failure . Isordil Sublingual tablets At the first signs of an anginal attack, place one or two tablets under your tongue
Isordil ® Sublingual Tablets Isosorbide Dinitrate Ingredients Active ingredient : 5 mg isosorbide dinitrate Inactive ingredients: • lactose........ diluent • starch........ direct compressible diluet , may act as binder, diluent and disintegrant have : + ve disintegration & - ve flowability • magnesium stearate........... act as a lubricant • microcrystalline cellulose ........... act as disintegrant • Erythrosine Lake............ colouring agent • CI 45430..................... colouring agent
Levsin ®/SL tablets _ Levsin ®/SL is one of the principal anticholinergic/antispasmodic components of belladonna alkaloids. * Drug Components : _ 0.125mg of Hyoscyamine sulphate " active ingredient ": treat a variety of stomach /intestinal problems such as cramps & irritable bowel syndrome . treat other conditions such as bladder and bowel control problems , cramping pain caused by kidney stones and gallstones . _ Inactive ingredients : FD&C blue #1 ... Coloring agent Lactose monohydrate ... Diluent Magnesium stearate ... Lubricant Mannitol ... Diluent & Sweetener Starch ... Disentigrant Stearic acid ... Lubricant
Ergomar ® Sublingual Tablets Ergomer is Prescriped for patient suffering from the migraine A migraine is a severe, painful headache that can be preceded or accompanied by sensory warning signs such as flashes of light, blind spots, tingling in the arms and legs, nausea, vomiting, and increased sensitivity to light and sound DESCRIPTION Ergotamine Tartrate Sublingual Tablets USP ( Active ingredient ) 2 mg Inactive Ingredients: Microcrystalline Cellulose ( Directly compressible diluent ), Natural Peppermint ( Flavor Powder ), Crospovidone ( super disintegrant ) , Saccharin Sodium ( sweetening Powder ), D&C Yellow #10 Lake( colour ), Magnesium Stearate ( lubricant ), FD&C Blue #1 Aluminum Lake( colour )
Saphris
Abstral * What is the drug used for ? _ Abstral is used for management of breakthrough pain in adult cancer patients (+18) who are already taking other opioid pain medicines around-the-clock for cancer pain. _ Abstral patient must be ( opioid tolerant ) Drug Components : _Fentanyl Citrate " active ingredient" ... Opioid agonist (Analgesic). Inactive Ingredients : Mg stearate ... Lubricant. Mannitol ... Diluent & Sweetener . silicified microcrystalline cellulose ... Diluent & Disintegrent ... Also, improve binding capability. croscarmellose sodium (sodium CMC) ... Disintegrent .