What is prodrug pharmacology?
A prodrug can be defined as a drug substance that is inactive in the intended pharmacological actions and is must to be converted into the pharmacologically active agent by metabolic or physico-chemical transformation.
What is a prodrug explain with example?
Prodrug: A precursor (forerunner) of a drug. A prodrug must undergo chemical conversion by metabolic processes before becoming an active pharmacological agent. For example, sulfasalazine is a prodrug. It is not active in its ingested form.
What are the types of prodrug?
There are two major types of prodrugs. These categories are based on how prodrugs are converted in the body: 1) Type I prodrugs turn into their active forms inside of cells. 2) Type II prodrugs turn into their active forms outside of cells, such as in blood or other fluids.
How strong is Tilidin?
Considered a low-to-medium-potency opioid, tilidine has the oral potency of about 0.2, that is, a dose of 100 mg p.o. is equianalgesic to approximately 20 mg morphine sulfate orally.
What are the applications of prodrug?
The use of a prodrug is to optimize the absorption. Digestion and Absorption , distribution, metabolism, excretion and unwanted toxicity Toxicity Dosage Calculation of the parent drug. There are three basic objectives in prodrug research. Conflict of Interest : Pharmaceutical, pharmacokinetic and pharmacodynamics.
Why is prodrug useful?
Prodrugs can be used to improve drug delivery or pharmacokinetics, to decrease toxicity, or to target the drug to specific cells or tissues. Ester and phosphate hydrolysis are widely used in prodrug design because of their simplicity, but such approaches are relatively ineffective for targeting drugs to specific sites.
Why are prodrugs used?
Who discovered prodrug?
It is important to ensure that the prodrug should be pharmacologically inactive, rapidly converted to its active drug and a non-toxic moiety [14, 15]. Nearly 55 years ago, Albert introduced the prodrug term for the first time in his book ‘selective toxicity’.
What is the difference between drug and prodrug?
Drugs can be metabolized by several tissues and organs, such as the kidneys, lungs and intestines, but the main site of metabolism is the liver, which is rich in enzymes. A prodrug is a medication that the body converts into a pharmacologically active drug after it is administered.
Who discovered prodrugs?
How is a prodrug formed?
Prodrug is a pharmacologically inactive derivative of an active drug and undergoes in vivo biotransformation to release the active drug by chemical or enzymatic cleavages. [1,2,3] A prodrug strategy is typically used when a pharmacologically active drug has poor solubility or permeability.
What is the application of prodrug?
The use of a prodrug is to optimize the absorption. Digestion and Absorption , distribution, metabolism, excretion and unwanted toxicity Toxicity Dosage Calculation of the parent drug.
Which is the earliest discovered prodrug?
Prontosil
Which is the earliest discovered prodrug? Explanation: Prontosil is the prodrug for the antibacterial agent sulfanamide in the body. It was the earliest prodrug discovered accidentally. Aspirin is the prodrug of salicylic acid used to reduce gastric irritation.
What is Valoron used for?
VALORON is indicated for the relief of acute, moderate to severe pain, and chronic cancer-related pain. CONTRAINDICATIONS: VALORON is contraindicated in patients with a history of hypersensitivity to this drug. It should not be used in conditions in which an increase in intracranial pressure may be dangerous.
Qual è il principio attivo della morfina?
La morfina è stato il primo principio attivo estratto da una fonte vegetale ed è uno degli almeno 50 alcaloidi di diversi tipi presenti nell’oppio. La morfina è generalmente contenuta in un 8-17 per cento del peso a secco dell’oppio, anche se può raggiungere il 26 per cento in alcune specie.
Quali sono gli effetti gastrointestinali della morfina?
Gli effetti gastrointestinali della morfina sono mediati dai recettori μ-oppioidi nell’intestino. Inibendo lo svuotamento gastrico e riducendo la peristalsi dell’intestino, la morfina riduce la velocità di transito intestinale.
Come si utilizza la morfina per il trattamento del dolore?
Trattamento del dolore. La morfina è utilizzata principalmente per il trattamento del dolore grave, sia acuto che cronico. Viene utilizzata anche per gestire il dolore causato dall’infarto del miocardio e per i dolori del parto. La durata del suo effetto analgesico è tra circa tre e sette ore.
Quali sono gli effetti della morfina sulla memoria?
Sono presenti pochi studi riguardo gli effetti della morfina sulle capacità motorie; un’elevata dose di morfina può compromettere il movimento delle dita e la contrazione isometrica (cioè il controllo motorio fine). La morfina può avere un impatto negativo sulla memoria, ma questi effetti sono minimi e transitori.