Table of Contents
- 1 How does sublingual route of drug administration bypass first pass metabolism in liver?
- 2 How much can be absorbed sublingually?
- 3 Do all drugs go through the liver?
- 4 What can be absorbed sublingual?
- 5 How effective is sublingual absorption?
- 6 Why sublingual route of drug administration directly entered in organ?
- 7 Why are sublingual and buccal drugs given sublingually?
- 8 What is the sublingual mucosa of the tongue?
How does sublingual route of drug administration bypass first pass metabolism in liver?
Alternative routes of administration, such as insufflation, suppository, intravenous, intramuscular, inhalational aerosol, transdermal, or sublingual, avoid the first-pass effect because they allow drugs to be absorbed directly into the systemic circulation.
Where is a sublingual drug administered?
The sublingual mucosa is the membrane of the ventral surface of the tongue. Sublingual administration of drug refers to the placement of drug under the tongue (Rehfeld et al., 2017). The sublingual route bypasses the first-pass metabolism and hence facilitates rapid absorption of the drug into the systemic circulation.
How much can be absorbed sublingually?
The bioavailability of a 5-mg sublingually administered dose is around 35\%. The bioavailability values of other doses were calculated from clinical data (Fig. 3). The bioavailability is more or less constant at low doses and goes down when the doses exceed around 5 mg.
How is sublingual nitroglycerin absorbed?
Nitroglycerin sublingual tablets should not be chewed, crushed, or swallowed. They work much faster when absorbed through the lining of the mouth. Place the tablet under the tongue or between the cheek and gum, and let it dissolve.
Do all drugs go through the liver?
Most drugs must pass through the liver, which is the primary site for drug metabolism. Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms. The liver’s primary mechanism for metabolizing drugs is via a specific group of cytochrome P-450 enzymes.
Do IV drugs pass through the liver?
Drugs that are administered orally (as opposed to intravenously, intramuscularly, sublingually, or transdermally) must first pass from the intestine to the liver before reaching the general circulation. Thus, for many drugs, much of the dose is reduced by xenobiotic metabolism before reaching the tissues.
What can be absorbed sublingual?
Many drugs are absorbed through sublingual administration, including cardiovascular drugs, steroids, barbiturates, benzodiazepines, opioid analgesics, THC, CBD, some proteins and increasingly, vitamins and minerals.
What is the most commonly administered sublingual medication?
Ideally, for a drug to be delivered sublingually, the drug should dissolve rapidly, produce desired therapeutic effects with small amounts of drug, and be tasteless. Examples of commonly prescribed sublingual tablets include nitroglycerin, loratadine, mirtazapine, and rizatriptan (Table 1-2).
How effective is sublingual absorption?
The absorption of the drug through the sublingual route is 3 to 10 times greater than oral route and is only surpassed by hypodermic injection. For these formulations, the small volume of saliva is usually sufficient to result in tablet disintegration in the oral cavity.
Is Nitroglycerin metabolized in the liver?
Metabolism: A liver reductase enzyme is of primary importance in the metabolism of nitroglycerin to glycerol di- and mononitrate metabolites and ultimately to glycerol and organic nitrate. Known sites of extrahepatic metabolism include red blood cells and vascular walls.
Why sublingual route of drug administration directly entered in organ?
Sublingual and buccal routes These drugs are not swallowed. The sublingual route is especially good for nitroglycerin, which is used to relieve angina, because absorption is rapid and the drug immediately enters the bloodstream without first passing through the intestinal wall and liver.
What is the difference between sublingual and oral route of absorption?
Sublingual and oral. Absorption is very quick, and higher drug levels are achieved in the bloodstream by sublingual routes than by oral routes because (1) the sublingual route avoids first-pass metabolism by the liver (Fig. 1-2 ), and (2) the drug avoids destruction by gastric juices or complexation with foods.
Why are sublingual and buccal drugs given sublingually?
When sublingual and buccal drugs are given. the drug needs to get into your system quickly you have trouble swallowing medication the medication doesn’t absorb very well in the stomach the effects of the drug would be decreased by digestion The cheek and area under the tongue have many capillaries, or tiny blood vessels.
Why is the sublingual route the most studied one?
The sublingual route is the most studied one because it is relatively more permeable and leads to rapid absorption of drugs with high acceptability (Şenel et al., 2012 ). The formulation of sublingual drugs uses two different designs: one in tablet form and the other in capsule.
What is the sublingual mucosa of the tongue?
The sublingual mucosa is the membrane of the ventral surface of the tongue. Sublingual administration of drug refers to the placement of drug under the tongue (Rehfeld et al., 2017). The sublingual route bypasses the first-pass metabolism and hence facilitates rapid absorption of the drug into the systemic circulation.