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drug delivery tutorials asnwers

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Name
Instructor
Course
Date
Drug Delivery Tutorials Answers
Tutor 1- Pharmacodynamics
Q1
Nonspecific targets act by exploiting the chemical and the physiochemical properties such as the sodium alginate and sodium bicarbonate while the specific targets act by therapeutically by binding to the peptides and proteins.
Q2
Pharmacodynamics refers to the effect of drugs on human body through the metabolic attraction.
Pharmacokinetics is the study on how drugs move in the body through metabolic process. Drugs in the body begin to exert any kind of effects before it is being absorbed in the system.
Tutor 2- Quantitative pharmacology
Q1
Affinity is how well a particular compound is held at the binding site while efficacy is the ability of a drug to produce a pharmacological response (Rmax) when it interacts with its receptor.
Q2
Potency in most cases involves both affinity and efficacy of the drugs on the binding sites of the receptor cells. Affinity is very strong on molecular compounds than the efficacy. Thus a drug binds to the receptors well when it is more affinity to it. Efficacy is the relationship of the receptor occupancy and its ability in initiating any response at the molecular cells.
Q3
Potency (for example EC50s), Maximal response (Rmax), partial and inverse agonist
Long drug concentration
Q4

Tutor 3 signal transduction and G-protein
Q1
Signal transducer is a process where there is a transmission of the chemical signal or physical signal through a cell which exhibits steps of molecular processes.

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In other words, it is the biological cellular mechanism which translates stimulus into the response in a cell.
Q2
Endocrine signaling comes from endocrine cells where there is the release of hormones that act on target cells in the body which are distant. Paracrine signaling comes from peregrine factors which are referred to as signaling molecules where cells produce signals which induce alterations in the cells nearby.
Anticrime signaling is from anticrime agents or hormonal cell secretion where cells secrete chemical messengers that link anticrime receptors on the common cells.
Q3

Q4
Complete the table
G-protein (a subunit) Effector enzyme Second messenger
G ẋ Adenylate cyclase( stimulation) EC 4.6.1.1
G ἰ Adenylyl cyclase cAMPG q Inositol triphosphateIP3,DAG,Ca2+
Tutor 4- Receptor kinase and kinase signaling cascades
Q1
Rhodopsin like GCPRs constituents the protein family with a wide range of roles, this include the anticrine and the endocrine process. Their structure has active ligands and the amino acid sequencing. Receptor tyrosine kinase is very affinitive to the cell surface receptors for many growth hormones. They are commonly identified in the human genome.

Q2
GPCRs play a role in the human body by increasing the action of the receptors in the body. It also binds a variety of the signals which are observed in the red blood cells. It consists of a single polypeptide that is globular in shape, and it is embedded in the plasma membranes. Its name implies that it interacts with the plasma membrane and the G-protein which binds with the extracellular loops forming the pockets which play a role in sending signals. RTK is also major cell receptors in the human body. It plays a role by binding a ligand to it and stimulates the receptors intrinsic protein (Bruno, 2014 p14). It is initiated the peptide-protein hormone which includes the growth factors (NGE) and the platelet-derived factors (PDGF). After binding, the ligand detaches itself from the receptor and get free to swim away or start to metabolize together with the receptor again. Some of the ligands will activate another receptor ligand to bind to the specific receptor, thus making none-specific interactions to fail into the realm.
Q3

Q4
Substrate for PI3K is the lipid kinase which is capable of phosphorylating the inositol rings found in the phosphoinositides. They are responsible for all coordination roles which includes proliferation and cell survival.
Tutor 5- Ion channels and transporters
Q1
Calcium ion is an example of an ion which is important in the regulation process of signal transduction within cells. Calcium ion acts as second messenger in the signaling pathways biochemically within cells.
Q2
Voltage-gated channels; these include ion channels of sodium and potassium of nerve terminals and nerve axons.
Intracellular ligand-gated ion channels; they include the ion channels involved in perception of sense and some ABC family ion channels which are normally activated by GCPRs indirectly.
Extracellular ligand-activated channels; they contain channels such as glycine receptor and GABA which are regulated by ligand neurotransmitters. They are usually identified according to the ligand they tend to bind to.
Q3
Voltage-gated ion channels open and close just depending on the gradient of voltage across the plasma membrane. When voltage is high they are opened but will close when the voltage is low. Lingad-gated ion channels depend on binding of ligands to the channel to open and close. Tension-gated ions channels hand open and close depending on the amount of mechanical stress in the surrounding.
Q4
Voltage-gated ion channels (VGICs) are important in modulation transmissions to do with neurons. They are responsible for quick signaling of electric charge within cells at shorter distances and often at longer distances. They are key proteins defining excitability of the cells.
Tutor 6- organization of autonomic nervous system
Q1

Q2
Complete the table (showing answers only)
Cranial nerve nuclei Innervations of sweat glands Thoracic and third lumbar segments Thoracic and third lumbar segments
short short long long
Parasympathetic ganglia Acetylcholine Acetylcholine Epinephrine and norepinephrine
Q3
Ca2+ and Na+ are integral in the release of neurotransmitter
Calcium and sodium are integral in the release of neurotransmitter where the accumulation of sodium in the synapse contributes to PTP through reduction of Na+ gradient. Ca2+ on the other hand, generates intrinsic processes where it acts as neuronal integration modulators to release transmitters.

Q4
Sweat glands have two parts of innervations being pre-ganglion and post-ganglion neurons. The neuron for sweat gland innervations is the only sympathetic postganglionic neuron which releases acetylcholine to act muscarinic receptor. This is what sets the sweat glands different from other neurons.
Tutor 7 cholinergic receptors
Q1
Acetylcholine is a receptor that is synthesized by the neurons by the choline acetyltransferase enzyme from the two main compounds of choline and acetyl-CoA. One of the examples of the central cholinergic are in the nucleus is Meynert basal forebrain.
The enzyme activity is also regulated by the products being inhibited. In addition, all the mass actions of the enzyme inhibit the production of Ach molecules which are found in the synaptic space.
Q2
In the human body, vesamicol inhibits the uptake of presynaptic vesicles, and its release is reduced. It also helps with rapid eye movement and sleep. The vesical drug prevents the uptake pump of the Ach in the synaptic vesicles. When it is released in the body, its effect is useful to both the experimental and the clinical functions. In addition, it increases the transmission of the NMJ Ach which is released by the AChR number such as the myasthenia gravis. When it is released in the body, it controls symptoms and treats the Alzheimer’s disease.
Q3
The main types of muscarinic receptors are G-Protein receptors and the nicotinic Ach receptors. The ACh receptors bind the acetylcholine and transmit its signal to the plasma membranes. The narcotic receptors are characterized by their interaction with the nicotine found in tobacco. They are the ligand-gated channels which form the plasma membranes and helps in mediating the fast signal transmission at the synapses. Muscarinic receptors water soluble which is derived from the mushroom which causes the substantial activation in the peripheral synaptic nervous system through the binding of the muscarinic AChRs.
Q4
Agonist drug includes acetylcholine. Its role is to activate the muscles and main neurotransmitter in the ANS. CNS projects from the basal forebrain to the cerebral cortex to the hypothalamus. It is one of the major neurotransmitters in the ANS.
The antagonist includes atropine. It is a medication which treats various nerve agents and the pesticide poisoning during slow heart rate. Another function is decreasing the production of saliva during surgery. It is an intravenous drug which is injected into the human muscles for it to perform the functions effectively.
Q5
Nicotinic antagonists include trimetaphan which characterized by hypertension in patients who are acute with aortic disease. It is a ganglion blocking agent which prevents the stimulation of postsynaptic and receptors by competing actively to the acetylcholine for the binding site. Another effect of the drug is vasodilatation and release of histamine in the body.
Agonistic include acetylcholine. It activates the muscles and main neurotransmitter in the autonomic nervous system (Bruno, 2014 p36). In the CNS, it projects from the basal forebrain to the cerebral cortex to the hypothalamus. It is one of the major neurotransmitters in the ANS.
Tutor 8- Adrenergic receptors
Q1
The synthesis of catecholamine in the human body involves some enzymatic procedures. Catecholamines are synthesized at the location where they are released in the nerves. This occurs at the terminals and the cell bodies. The enzyme that is involved in the synthesis of catecholamines is tyrosine hydroxylase (TH). It is a catalyst for the conversion of tyrosine and molecular oxygen substrates to dihydroxy-l-phenylalanine (L-DOPA).
Q2
Vesicular monoamine transporters are important because they transport neurotransmitters of monoamine into the vesicles. The vesicles then later release neurotransmitters into synapses which come in the form of chemical messages to the neurons of postsynaptic action. The drugs associated with the inhibition of monoamine transporters include psychostimulants such as cocaine and amphetamine drugs.
Q3
Monoamine oxidase (MAO) is pharmacologically targeted to regulate activities of the central nervous system and play a crucial role in the pathogenesis of disorders of depression and human neurodegenerative problems. Monoamine oxidase is simply an anti-depressive compound used in medication.
Q4
Adrenergic receptors include alpha, beta 1 and beta two receptors. The stimulation of alpha receptors which are located in the arteries causes constriction of arteries hence increasing blood pressure blood flow to the heart. Beta 1 receptors are located in the heart. The Stimulation of beta one receptors in most increases heart rate and the contraction strength of the heart.
Beta 2 receptors are located n the bronchioles. Their stimulation, on the other hand, causes widening of bronchioles to pass more air in and out during breathing process. They also help in the dilation of vessels of skeletal muscles.
Q5
Clonidine is a common medication for treating blood pressure and hyperactivity disorders. It is an example of α-adrenoceptor. Doxazosin is a drug which is taken orally for treating hypertension. It is given in form of mysylate. It is an example of α-adrenoceptor antagonist.
Example of β-adrenoceptor agonist includes dobutamine. It is a sympathetic drug used for treating heart failures and cardiogenic shock. It has a mechanism of β1 receptors in the nervous system.
Example of β-adrenoceptor antagonist include metoprolol and acebutolol
Tutor 9 Adrenergic and Non-cholinergic receptors NANC Receptor
Q1
The GABAA receptor is a gated ligand ion on the Cys-loop family which includes the nicotinic acetylcholine. The GABAA receptors have the alpha, beta and the gamma subunits which harbor the main hetero-oligomer constituents of the portion of it. The GABAA receptor mediated transmission for tuning the neuronal networks, and the generation of the rhythmic and the neuronal activities. Its main function is to reduce the inhibition in favor of the hyper excitability which results in rhythmic discharges. These mechanisms are used in determining the abundance of the subunits which compose of the GABAA receptors in the given brain cells.
Q2
Fluoxetine is one of the selective serotonin reuptake inhibitors, and it does not inhibit the norepinephrine and the dopamine reuptake in the therapeutic doses. Thus, both the dopamine and the norepinephrine contribute to the antidepressant action of the fluoxetine in human supratherapeutic.
Q3
The enteric nervous system (ENS) controls the effector systems of the entire digestive tract. It consists of the musculature, secretory glands, and the blood vessels (Bruno, 2014 p20). The main function of the circuits is to determine the generation of the action potentials which are found in the single neurons and the chemical transmission which comes into contact with the synapses. The enteric microcircuits are specialized in the digestive tract with many of the synaptic sites where all the information is transmitted. .
In both the brain and the spinal cord, the enteric circuitry involves processing of information and the generation of patterns in the signal which helps in determining the timing of the behaviors in the human body system.
Q4
Dopamine is synthesized mainly in areas of the central and the peripheral nervous system. It is also synthesized in areas of the hypothalamus; dopamine is produced by chromaffin cells and the caudate nucleus found in the brain. Dopamine is derived from the amino acid called tyrosine. It is one of the main agents used in the formation of the dopamine at a limiting rate.
Q5
The active metabolites of clopidogrel selectively inhibit the main binding of the adenosine diphosphate (ADP) to the platelet P2Y12 receptors. Its main function is to, mediate the activation of glycoprotein. It also functions by inhibiting the platelets aggregation when the action is irreversible. The mode of action of the clopidogrel is formation of a blood clot inside the blood vessel. This kind of medication can easily cause an individual to bleed or be bruised easily. An active metabolite is not when not isolated from the system becomes responsible for medication activity. Thus the platelet aggregation is induced by the agonists apart from the ADP which is also inhibited by blocking its amplification in the platelets activation which is done by ADP. Therefore, clopidogrel is not inhibited by phosphodiesterase.
Tutor 10 Inflammatory y mediators
Q1
Inflammatory mediators are substances which initiate and regulate all the inflammatory reaction in the body. The main inflammatory mediators are plasma proteins, lipid products, cytokines and the products of complement activation. All the active inflammatory mediators are only produced in response to various stimuli such as the microbial products. One of the mediators can be stimulated to release complement activation which in turn releases histamine and the cytokines (Bruno, 2014 p24). Histamine helps in response to physical injuries and antibodies mediated which plays a role in hypertensive reactions. In addition, histamine causes dilation of the arterioles and causes and increase in permeability of the veins. It also increases the vascular permeability by producing all the inter-endothelial gaps in the veins.
Serotonin is a preformed mediator. It is found in platelets and neuroendocrinal cells such as GIT. Its core function is acting as a neurotransmitter. Arachidonic Acid metabolites are a lipid mediator which found in membrane phospholipids. It stimulates all the vascular and the cellular reactions.
Q2
Eicosanoid is a class of compounds such as thromboxanes and the leukotrienes which are derived from polyunsaturated fatty acids. They play a role in cellular activities.
Q3
Eicosanoids consist of prostaglandins, thromboxanes, leukotrienes, and lipoxins. All this are identified as prostanoids. Eicosanoids are synthesized by mammalian cells except for the erythrocytes. The eicosanoids function locally at a site of synthesizes by the receptor-mediated G-protein which is linked to the pathways. The cyclic pathway is initiated by prostaglandin synthesis. This enzyme has two main activities, cyclooxygenase, and the peroxides. The linear pathway is observed through the actions of the arachidonate by forming various compounds.
Q4
NSAIDs work by reducing the production of prostaglandins. They also take part in protecting the lining of the stomach and the intestines. NSAIDs block both the COX-1 and COX-2. It is also used in treating all the conditions which cause inflammation and mild pains such as headaches cold and sports injuries.
Q5
Cetirizine is one of the non-sedating antihistamines which work by blocking histamine receptors in the body cells. It acts on highly selective antagonist of the histamine H1 receptors.
Antihistamine activity of Cetirizine works in both the vivo and ex vivo animal’s model by showing the negligible ant cholinergic and the serotonergic activity. It is not significantly occupied in the cerebral H1receptors.

Work Cited
Dr. Bruno Sil dos Santos. Autonomic computing. (2014). London , springer

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